GSK778 (iBET-BD1) potently inhibits numerous cancer cells proliferation, inducing cell cycle arrest and apoptosis. Applications Products Services Documents Support. In humans, 61 bromodomains, each composed of ∼110 amino acids forming four antiparallel α helices (αZ, αA, αB, and αC) and two hydrophobic (ZA and BC) loops, in 46 different proteins have been described. GSK778 is a potent and selective inhibitor of BD1 bromodomain such as BRD2 BD1 (IC50s = 75 nM), BRD3 BD1 (IC50s = 41 nM), BRD4 BD1 (IC50s = 41 nM), and BRDT BD1 (IC50s = 143 nM). ≥98% (HPLC) All Photos (1)GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. 2451862-42-1: Formula: C 30 H 33 N 5 O 3: Formula Wt. CAS# 2451862-42-1. 7 B) indicated that GSK778 maintains all of the critical interactions of I-BET151 with BRD4-BD1, including the hydrogen bonding interaction of the 3,5-dimethylisoxazole moiety with the conserved Asn140, the hydrophobic interaction of the aryl ring of the α-methylbenzyl group with the. Available to order from Sigma-Aldrich. Molecular Formula: C30H33N5O3. Chemical probes are cell-active, selective, highly validated research tools that can be used to decipher the biology of their target. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. $21. View and buy high purity iBET-BD1 | GSK778 from AOBIOUS, the leading supplier of life science reagents. Not for human use. CAS Number: 2451862-42-1. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. Not for human use. GSK778 reduces the production of anti-keyhole limpet. Potency in Cells and Cellular Target Engagement: GSK778 engages the target in HEK293 cells: pIC50 = 7. Applications Products Services Documents Support. GSK778 Hydrochloride. Fax: +1 510. BD1 selective inhibitors, such as GSK778, MS-436, Olinone, and BI-2536, as well as the BD2 selective inhibitors RVX-208, RVX-297, GSK046, and ABBV-744 have been produced. SML3234. Email. In almost half of hepatocellular carcinoma (HCC) cases, the Akt pathway is activated. All Photos (1) Documents. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. ≥98% (HPLC) All Photos (1)MS40224, and GSK77825. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Before sharing sensitive information, make sure you’re on a federal government site. 77 The basic structure of BET proteins is comprised of. SML3234. All Photos (1) SML3234. Open in a. Copy Link. 3; Cell. VI EN. All Photos (1) SML3234. By Louis Gilman. ZA EN. Recombinant IL-1β (Peprotech, Cranbury, NJ) was reconstituted RPMI at 0. 5), is a highly selective BD1 inhibitor (BRD4(1), IC 50 = 41 nM) with a 143-fold selectivity over BD2. GSK778. ≥98% (HPLC) All Photos (1)GSK778 (iBET-BD1) is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. 451491-47-7 CTB (Cholera Toxin B subunit) is an activator of p300 histone acetyltransferase and induces apoptosis in MCF-7 cells. The distinct families are. Products are for research use only. SML3234. Endoplasmic Reticulum Stress Modulator (ERSM) Epigenetics Resch Products. GSK778 Hydrochloride. Applications Products Services Documents Support. $21. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. 00. All Photos (1) Documents. WGK. Available to order from Sigma-Aldrich. ID EN. Modukuri a,1, Zhifeng Yu , Zhi Tan , Hai Minh Tab,1, Melek Nihan Ucisik a. COO/ COA. Phylogenetic tree of the human bromodomain-containing protein subgroups. All Photos (1) Documents. GSK778 (iBET-BD1) is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. : 2451862-42-1. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. (D) Venn diagram showing the overlap between top DCP hits in tumor organoids (ERKi) and normal organoids (BAY-293, BI99179, GSK778, GSK789). In contrast to other reported domain-selective molecules, these compounds showed little binding to bromodomains. GSK778 (iBET-BD1) potently inhibits numerous cancer cells proliferation, inducing cell cycle arrest and apoptosis. GSK778 (iBET-BD1) potently inhibits numerous cancer cells proliferation, inducing cell cycle arrest and apoptosis. ≥98% (HPLC)Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). The structures of the two predominant metabolites (M4 and M5) of RVX-208, observed both in in vitro human and animal liver microsomal incubations, as well as in plasma from animal in vivo studies, were determined. CTB ( Cholera Toxin B subunit ) Catalog No. MS EN. 4 D and E) shows that our BD1-selective and BD2-selective DECL-derived inhibitors each occupy the same KAc pocket as GSK778 but also access adjacent grooves that differ between the two domain types. Open in a separate window. ≥98% (HPLC)GSK778 ( iBET-BD1 ) Catalog No. • GSK778 exhibits >130-fold BD1 selectivity over BD2 due to BD1 Asp144/His433 displacement (Kharenko et al. Available to order from Sigma-Aldrich. On the basis of sequence homology, BCPs are classified into eight different subgroups (families). S1F, and table S1). SML3234. Drugs that inhibit both bromodomains equally have shown efficacy in certain malignant and inflammatory conditions. To explore the individual functional. 5 (LPS-PBMC assay) ≤ 10 µM. GSK778 (iBET-BD1) is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Available to order from Sigma-Aldrich. Domain-Selective Targeting (BD1 or BD2 Targeting) The BET protein family of BCPs comprise the ubiquitously expressed BRD2, BRD3, and BRD4 and the testis-restricted BRDT, all of which harbor two highly conserved tandem bromodomains, BD1 and BD2,. The two tandem bromodomains of the BET proteins enable chromatin binding to facilitate transcription. COO/ COA. 125 nM (MV-4−11 cells) ≤. ksg@ahjnirp. (B). BET BD1 related products. Inhibition of BET bromodomains by small molecule inhibitors has emerged as a promising therapeutic strategy for cancer. Figure 4. IC₅₀ & Target BRD2 BD1 75 nM (IC50) BRD3 BD1 41 nM. GSK778 Hydrochloride. GSK778 and GSK046 are termed iBET-BD1 and iBET-BD2 respectively. GSK778 (iBET-BD1) is a potent and selective inhibitor of the BD1 bromine domain of the BET protein,IC50 The values are 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4. GSK778 (iBET-BD1) is a potent and selective inhibitor of bromodomain (BRD) BD1. SML3234. Storage Class Code. GSK778 phenocopies the. GSK778 Hydrochloride. 1. S1F, and table S1). Drug Formulation: This drug may be formulated in DMSO. RVX-297 is a 4-quinazolinone derivative related to RVX-208 with an alkylpyrrolidine side chain off the di-methyl substituted phenyl ring (Fig. AA Blocks. Copy Link. Miransertib is an Orally Active Akt Inhibitor for Cancer and Infection Research. The oldest compound, RVX-208 based on a quinazolinone chemical core, exhibited a selectivity of 20-fold with K D values of 4100 nMComprar GSK778 hydrochloride na CymitQuimica a partir de 187,0 €I-BET151 (GSK1210151A), iBET-BD1 (GSK778) and iBET-BD2 (GSK046) were provided by GlaxoSmithKline plc (GSK, London, UK). Flight status, tracking, and historical data for N778SK including scheduled, estimated, and actual departure and arrival times. 27,42 The second-generation BRD4 inhibitors are mainly synthesized by proteolysis targeting chimera (PROTAC) technology. their selectivity. Email. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. Available to order from Sigma-Aldrich. Instead, a unique effect of BD2-selective antagonism was revealed with GSK046, affecting the induction of gene expression more so than the expression of steady-state genes, in contrast to. Miransertib target all three Akt isoforms by blocking…. 02:05PM IST Netaji Subhash Chandra Bose Int'l - CCU. Applications Products Services Documents Support. First of all, GSK778 (iBET-BD1) is a potent and selective inhibitor of bromodomain (BRD) BD1. GSK778. Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months). All. SML3234. Applications Products Services Documents Support. Copy Link. COO/ COA. Selectivity profile of I-BET151, iBET-BD1 (GSK778) and iBET-BD2 (GSK046). Immunoblots. Inhibitor/agonist potency: goal is < 50 nM (IC 50, K D) Surpasses criterion: :BET mutant TR-FRET assay: BRD2 (BD1) pIC 50 = 7. SML3234. In contrast to other reported domain-selective molecules, these compounds showed little binding to bromodomains. WGK 3. , 2010), I-BET762 (Nicodeme et al. For research use only. comThe calculations of the energy contributions of individual residues demonstrate that residues corresponding to (BD1, BD2) generate significant energy difference in binding of SG3-179, GSK778, and. 8905. All products from TargetMol are for Research Use Only. COO/ COA. Available to order from Sigma-Aldrich. GSK778 (iBET-BD1) potently inhibits numerous cancer cells proliferation, inducing cell cycle arrest and apoptosis. GSK778 (iBET-BD1) is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. GSK778 hydrochloride | C30H34ClN5O3 | CID 168013350 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological. All Photos (1) Documents. GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. Preis und Verfügbarkeit anzeigen. Applications Products Services Documents Support. GSK778 is a potent and selective inhibitor of bromodomain (BRD) BD1, with IC50s of 75 nM (BRD2 BD1). HR EN. Email. COO/ COA. To explore the individual functional contributions of BD1 and BD2 in biology and therapy, selective BD1 and BD2 inhibitors have been developed: GSK778 and GSK046 (termed iBET-BD1 and iBET-BD2, respectively) . GSK778. HY-136570 10mg GSK778 CAS: 2451862-42-1 GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. (A) Schematic of the BET Bromodomain proteins and chemical structures. Lymphoma Non. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. Available to order from Sigma-Aldrich. GSK778 Hydrochloride. Available to order from Sigma-Aldrich. Recently, inhibitors were developed that selectively target the first (BD1) and second (BD2) bromodomain of the BET proteins (iBET‐BD1 (GSK778) and iBET‐BD2 (GSK046)). GSK778 offers a superior survival advantage to iBET-BD2 in the aggressive MLL-AF9 AML model. Please continue to check back for new reviews and commentary. COO/ COA. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models. GB EN. Catalog Number: AA01KEG7. amni) under a material transfer agreement with GSK. 27, 42. However, many compounds reported in the literature and routinely studied in biomedical research lack the potency and selectivity. EG EN. 1B, fig. All Photos (1) Documents. $79. Their affinities for the individual bromodomains of the BET family were initially determined by TR-FRET (Fig. 10 µM; GSK791. 999. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. Herein, GSK778 and GSK046 are referred to as iBET-BD1 and iBET-BD2, respectively. Copy Link. Instead, a unique effect of BD2-selective antagonism was revealed with GSK046 affecting the induction of gene expression more so than the expression of steady-state genes, in contrast to GSK778 . SGC Toronto. Sigma-Aldrich. GM6001. The two tandem bromodomains of the BET. GSK778 hydrochloride hydrochloride phenocopies the effects of pan-BET inhibitors in cancer models[1]. Applications Products Services Documents Support. COO/ COA. Available to order from Sigma-Aldrich. Coordinates and structure factors have been deposited in the Protein Data Bank (PDB) with identification code 6SWN, 6SWO, 6SWP and 6SWQ. 5 upper limit of normal (ULN) Total bilirubin < 1. Copy Link. GSK778. orgGSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Available to order from Sigma-Aldrich. Recently, inhibitors were developed that selectively target the first (BD1) and second (BD2) bromodomain of the BET proteins (iBET-BD1 [GSK778] and iBET-BD2 [GSK046]). Molecular Formula: C30H33N5O3. , Suite 700 Toronto, ON, M5G 1L7 Canada +1 416-946-0237. Molecular Weight: 511. K. 6SWN: N-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH iBET-BD1 (GSK778) PDB ID: 6SWN Download: MMDB ID: 192697: PDB Deposition Date: 2019/9/22: Updated in MMDB: 2021/02: Experimental Method: x-ray diffraction. The second-generation BRD4 inhibitors are mainly synthesized by proteolysis targeting chimera (PROTAC) technology. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. GSK778 (iBET-BD1) is an analogue of I-BET151 with good potency against BET BD1 (IC 50 = 40 nM) and similar selectivity to LT052 (150-fold) over BD2 [48]. GSK789 was derived from a series of naphthyridone ATAD2 inhibitors. SynTEF1, a prototype synthetic genome reader/regulator (SynGR), was designed to target GAA triplet repeats and restore the expression of frataxin (FXN) in Friedreich’s ataxia patients. Email. All Photos (1) Documents. 6swo: c-terminal bromodomain of human brd2 with ibet-bd1 (gsk778)BRD3. TW EN. Available to order from Sigma-Aldrich. Available to order from Sigma-Aldrich. SML3234. Available to order from Sigma-Aldrich. WGK. HY-136570 25mg GSK778 CAS: 2451862-42-1 GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. Email. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. 511. MCP-1 in LPS-stimulated PBMCs: 1000 <1: 32193360. The calculations of the energy contributions of individual residues demonstrate that residues corresponding to (BD1, BD2) generate significant energy difference in binding of SG3-179, GSK778, and. Email. WGK 3. The calculations of the energy contributions of individual residues demonstrate that residues corresponding to (BD1, BD2) generate significant energy difference in binding of SG3-179, GSK778, and. All Photos (1) Documents. Despite their profound preclinical efficacy, the clinical utility of pan-inhibitors is limited due to observed cytotoxicicities. 1B, fig. iBET-BD1 showed a selectivity of ≥130-fold for BRD4 BD1, and iBET-BD2. Storage Class Code. However, recent reports of potent and selective pan-BET BD1 and pan-BET BD2 inhibitors have been reported including ABBV-744, 21 GSK778, and GSK046. The addition of olinone to oligodendrocyte progenitor cells demonstrated biological effects divergent from pan-BET inhibition. Storage Class Code. ABBV-744 is highly selective for BD2 of BRD2, BRD3 and BRD4, 64 exhibiting several hundred-fold higher affinity for the BD2 over BD1. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models. Drug Formulation: This drug may be formulated in DMSO. ChemScene Provide GSK778(CAS 2451862-42-1)In-stock or Backordered impurities,Bulk custom synthesis,Formular C30H33N5O3,MW 511. ≥98% (HPLC)GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. GSK778 (iBET-BD1) potently inhibits numerous cancer cells proliferation, inducing cell cycle arrest and apoptosis. All Photos (1) Documents. GSK778 reduces the production of anti-keyhole limpet. GSK778 was found as a BD1 selective inhibitor with 130 times higher affinity for BD1 than BD2 5. . ChemicalBook provide Chemical industry users with GSK778 Boiling point Melting point,GSK778 Density MSDS Formula Use,If You also need to GSK778 Other information,welcome to contact us. However, many compounds reported in the literature and routinely. 2′,3′-Didesoxycytidin. In addition, while GSK778 phenocopied I-BET151 in terms of antiproliferative effects on a range of human cancer cells, GSK046 was less effective. WGK. 6SWN, 6SWO, 6SWP, 6SWQ. GSK778 is a potent and selective inhibitor of bromodomain (BRD) BD1, with IC50s of 75 nM (BRD2 BD1). Applications Products Services Documents Support. Copy Link. Catalog No. Their affinities for the individual bromodomains of the BET family were initially determined by TR-FRET (Fig. ≥98% (HPLC) All Photos (1)GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. 5. Forodesine hydrochloride ≥98% (HPLC); Synonyms: 7-[(2S,3S,4R,5R)-3,4-Dihydroxy-5-(hydroxymethyl)-2-pyrrolidinyl]-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one, hydrochloride salt,BCX-1777 HCl,ImmH HCl,Immucillin-H HCl; find Sigma-Aldrich-SML3378 MSDS, related peer-reviewed papers, technical documents, similar products & more at Sigma. 1 Among these, bromodomain and extraterminal (BET) proteins constitute a unique group with four family members, bromodomain-containing protein 4 (BRD4), BRD3, BRD2, and. We do not sell to patients. Selectivity profile of I-BET151, iBET-BD1 (GSK778), and iBET-BD2 (GSK046). SML3234. COO/ COA. BRD4 inhibitors effectively penetrate the blood-brain barrier and target glioma tumor tissues but have little effect on normal brain tissues. M28843 CAS No. All Photos (1) SML3234. 6 GSK789 (BD1) IC50= 125 nM (MV-4−11 cells) <10: GSK791. GSK778 (iBET-BD1) potently inhibits numerous cancer cells. Coordinates and structure factors have been deposited in the Protein Data Bank (PDB) with identification codes 6SWN, 6SWO, 6SWP, and 6SWQ. GSK778 phenocopies the. The calculations of the energy contributions of individual residues demonstrate that residues corresponding to (BD1, BD2) generate significant energy difference in binding of SG3-179, GSK778, and. Flight history for Vistara flight UK778. Binding free energy predictions suggest that entropy changes, electrostatic interactions, and van der Waals interactions are key factors in the selective binding of BD1 and BD2 by SG3-179, GSK778. GSK778 Hydrochloride. ChemicalBook 致力于为化学行业用户提供FREEBASE的性质、化学式、分子式、比重、密度,同时也包括FREEBASE的沸点、熔点、MSDS、用途、作用、毒性、价格、生产厂家、用途、上游原料、下游产品等信息。 Recently, Gilan et al. Safety Information. Herein, GSK778 and GSK046 are referred to as iBET-BD1 and iBET-BD2, respectively. The authors found that in mouse models of various cancers, BD1 inhibition is reminiscent of pan-BET inhibi-tion. Copy Link. Copy Link. 5 GSK778 (BD1) ↓. Herein,. T9703 CAS 2451862-42-1 GSK778 is a potent and selective inhibitor of BD1 bromodomain such as BRD2 BD1 (IC50s = 75 nM), BRD3 BD1 (IC50s = 41 nM),. Safety Information. GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. COO/ COA. GSK778 Hydrochloride. *. 1iBET-BD1 (GSK778) Following the initial report of the biological activity of iBET-BD1 and iBET-BD2, 19 Wellaway et al. 2h 41m. Request PDF | A Simple Electrostatic Model for the Hard-Sphere Solute Component of Nonpolar Solvation | We propose a new model for estimating the free energy of forming a molecular cavity in a. FRAP, BAZ2B: 1000 3:. For research use only. Some, such as ABBV-744 and GSK778, are optimized for greater selectivity for one of two distinct BET protein bromodomains in an effort to improve therapeutic indices [55, 56]. Shelf Life: >2 years if stored properly. , 2020), which is accordant to a previous reported BD1-specific inhibitor (Ma et al. Available to order from Sigma-Aldrich. Serum alanine aminotransferase (ALT)/aspartate aminotransferase (AST) < 2. Discovery of potent BET bromodomain 1 stereoselective inhibitors using DNA-encoded chemical library selections Ram K. Copy Link. GSK778 Hydrochloride. ≥98% (HPLC)HY-136570 10mg GSK778 CAS: 2451862-42-1 GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. R (moc. CAS Number: 2451862-42-1. Find here details of companies selling GSK778, for your purchase requirements. First of all,. 39 Proteolysis targeting chimeras. ≥98% (HPLC)We would like to show you a description here but the site won’t allow us. 6swn: n-terminal bromodomain of human brd4 with ibet-bd1 (gsk778)GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. Hazard identification. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Available to order from Sigma-Aldrich. This approachGSK778 (iBET-BD1) is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. (B) Compound binding to the individual bromodomains of BD1 (orange) and BD2 (cyan) of BET tandem bromodomains in TR-FRET assays. Additionally, while GSK778 phenocopied I-BET151 in terms of anti-proliferative effects on a range of human cancer cells, GSK046 was less effective. 10 µM; GSK791. 1B, fig. GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC 50 s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Related Post. ≥98% (HPLC)GSK778 (iBET-BD1) is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. All Photos (1) Documents. Coordinates and structure factors have been deposited in the Protein Data Bank (PDB) with identification code 6SWN, 6SWO, 6SWP and 6SWQ. GSK778 (iBET-BD1) is a strong BD1 bromodomain inhibitor of the BET proteins, with IC50 value of 75 nM for BRD2 BD1, 41 nM for BRD3 BD1, 41 nM for BRD4 BD1, and 143 nM for BRDT BD1. You can also browse global suppliers,vendor,prices,Price,manufacturers of GSK778(2451862-42-1). The nitrogen atom in pyrrolidine can form water-mediated hydrogen bonds with Asp144 (replaced with His433 in BRD2(2)) and Asp145, which may be. nM, SPR BRD4 (BD1): pKd= 8. SML3234. In addition, recent studies have shown that selective. Email. Europe PMC is an archive of life sciences journal literature. 6147. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. Email. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. Where indicated, 1 μm GSK778 or GSK046 or carrier (DMSO) were added at the same time as LPS. Applications Products Services Documents Support. GSK789 was derived from a series of naphthyridone ATAD2 inhibitors. 1% Tween-20 and incubated with. 125 nM (MV-4−11 cells) ≤. COO/ COA. T9703 CAS 2451862-42-1. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. 09-Sep-2023. All Photos (1) Documents. GSK778 Hydrochloride. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. 4 D and E) shows that our BD1-selective and BD2-selective DECL-derived inhibitors each occupy the same KAc pocket as GSK778 but also access adjacent grooves that differ between the two domain types. GSK778 is a Potent and Selective Inhibitor of BET BD1 . Applications Products Services Documents Support. Comparison of the binding modes of CDD-956 with BD1, CDD-1302 with BRDT-BD2 , and iBET-BD1 (GSK778) with BRD4-BD1 (Fig. GSK778 Hydrochloride. DNA/RNA Synthesis Inhibitor/Blocker. We would like to show you a description here but the site won’t allow us. ChemicalBook 致力于为化学行业用户提供FREEBASE的性质、化学式、分子式、比重、密度,同时也包括FREEBASE的沸点、熔点、MSDS、用途、作用、毒性、价格、生产厂家、用途、上游原料、下游产品等信息。GSK778 phenocopied the effects of pan-BET inhibitors in cancer models. GSK778 is a potent and selective inhibitor of BD1 bromodomain such as BRD2 BD1 (IC50s = 75 nM), BRD3 BD1 (IC50s = 41 nM), BRD4 BD1 (IC50s = 41 nM), and BRDT BD1 (IC50s = 143 nM). Of these, only ABBV-744 and two molecules described within the article, GSK778 (iBET-BD1) and GSK046 (iBET-BD2) showed appreciable selectivity. 33DFTG (TD139) $21. In human whole blood and MV-4–11 cells, selective inhibition of GSK778 against BD1 retains the anti-inflammatory and antiproliferative phenotype features of pan-BET inhibition. • RVX-208 (Apabetalone), which is a BD2-selective BETi showing 30-to. Europe PMC is an archive of life sciences journal literature. Introduction. R (moc. This approach implicates the use of. MH EN. MR EN. (B) Compound binding to the individual bromodomains of BD1 (orange) and BD2 (cyan) of BET tandem bromodomains in TR-FRET assays. • Xanthine derivatives bind to BD1 with 10 times the affinity (Gilan et al. GSK046 (iBET-BD2) es un inhibidor de bromodominio BD2 potente, selectivo y oralmente activo de las proteÍnas BET, con IC50 de 264 nM (BRD2 BD2), 98 nM (BRD3 BD2), 49 nM (BRD4 BD2) y 214 nM (BRDT BD2), respectivamente. Email. Using these molecules, Gilan et al. GSK778 offers a superior survival advantage to iBET-BD2 in the aggressive MLL-AF9 AML model. Storage Class Code. BRDT. GSK778 (iBET-BD1) is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Applications Products Services Documents Support. These challenging conclusions were drawn based on the similarity of antitumor effects as well as the gene expression spectrums between BD1-selective compound iBET-BD1 (GSK778) and the pan-BET inhibitor iBET-151 (Gilan et al. SERP Rating Probe GSK778 is in the process of SERP review. Their affinities for the individual bromodomains of the BET family were initially determined by TR-FRET (Fig. Pan-BD1 inhibitors (which have higher inhibitory activity for BD1 than BD2 of BET proteins) are comparable to pan-BD inhibitors, such as MS436, 59 Olinone, 60 MS402, 61 3U, 62 GSK778, 19 ZL0516, 63 UMN627, 64 and GSK789. CAS: 2451862-42-1 (free base) Chemical Name: GSK778 2HCl; 4-(2-(Methoxymethyl)-1-((R)-1-phenylethyl)-8-(((S)-pyrrolidin-3-yl)methoxy)-1H. GSK778 inhibits proliferation, induces a cell cycle arrest and Apoptosis . WGK 3. ChemScene Provide GSK778(CAS 2451862-42-1)In-stock or Backordered impurities,Bulk custom synthesis,Formular C30H33N5O3,MW 511. Available to order from Sigma-Aldrich. A320.