I-BET151

  Cat. No.:  DC5183   Featured
Chemical Structure
1300031-49-5
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Field of application
I-BET151 (GSK1210151A) is a novel selective BET inhibitor for BRD2, BRD3 and BRD4 with IC50 of 0.5 μM, 0.25 μM, and 0.79 μM, respectively.
Cas No.: 1300031-49-5
Chemical Name: 7-(3,5-dimethylisoxazol-4-yl)-8-methoxy-1-((R)-1-(pyridin-2-yl)ethyl)-1H-imidazo[4,5-c]quinolin-2(3H)-one
Synonyms: IBET151,I-BET-151,I BET 151,IBET-151,IBET 151,GSK1210151A,GSK-1210151A,GSK 1210151A
SMILES: CC1=C(C(=NO1)C)C2=C(C=C3C(=C2)N=CC4=C3N(C(=O)N4)[C@H](C)C5=CC=CC=N5)OC
Formula: C23H21N5O3
M.Wt: 415.44
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: I-BET151 is a BET bromodomain inhibitor which inhibits BRD4, BRD2, and BRD3 with pIC50 of 6.1, 6.3, and 6.6, respectively.
In Vivo: I-BET151 (GSK1210151A) demonstrates low blood clearance in the rat (~20% liver blood flow) and good oral systemic exposure which resulted in good oral bioavailability. High clearance is observed in the dog (~95% liver blood flow). The systemic exposure in the dog is low, resulting in a poor oral bioavailability of 16%. The high blood clearance in dog correlates well with the high intrinsic clearance observed in dog microsomes and hepatocytes, whereas the low intrinsic clearances seen in rat and mouse (mouse IVC 1.6 mL/min/g; CLb 8 mL/min/kg) correlate with lower in vivo blood clearances in these species. Due to the low systemic exposure observed in the dog, I-BET151 is investigated in the mini-pig as a potential second species for toxicological evaluation where it showed low clearance (~32% liver blood flow) and good bioavailability (65%)[1]. In an in vivo model of subcutaneous myeloma, I-BET151 (50 mg/kg)-treated mice has four- to five fold smaller myeloma tumors (P<0.001) and a significantly reduced rate of tumor size doubling than vehicle-treated mice (P<0.001)[2].
In Vitro: I-BET151 (GSK1210151A) causes a significant dose- and time-dependent decrease in the proportion of myeloma cells in S/G2 phase at 24, 48, and 72 hours. The most pronounced effect is observed at 72 hours in all 6 myeloma cell lines, starting at 100 nM. Dual Ki67/propidium iodide staining confirmed that the majority of live cells resided in the G0 phase after treatment with I-BET151 at 1 μM for 72 hours commensurate with a dose- and time-dependent decrease in cell proliferation and abrogation of bromodeoxyuridine incorporation[2].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
DC70466 GSK549 GSK549 (GSK-549) is a potent, highly selective, BD2 domain-selective BET inhibitor with pIC50 of 7.8 (BRD4 BD2), 1150-fold selectivity over BD1.
DC11261 ZL0420 ZL0420 is a potent, highly selective BRD4 inhibitor with IC50 of 27 and 32 nM for BRD4-BD1 and BRD4-BD2, respectively.
DC8261 (-)-JQ-1 The (-)-JQ1 stereoisomer has no appreciable affinity to BET bromodomains,it is the negative control of +JQ-1.
DC8320 RVX-208 RVX-208(RVX 000222) is a small molecule that increases apolipoprotein A-I and high-density lipoprotein cholesterol in vitro and in vivo; is a BET bromodomain antagonist.
DC10786 PLX51107 PLX51107 is a novel BET inhibitor with a unique binding mode in the acetylated lysine binding pocket of BRD4 that differentiates it from other compounds under investigation.
DC8291 PFI-4 PFI-4 is a potent and selective BRPF1 bromodomain inhibitor (IC50 = 80 nM).
DC7649 PFI-3 PFI-3 is a novel potent, selective and cell permeable inhibitor of SMARCA4 and PB1(5) bromodomains with IC50 ~ 89 nM and 48 nM respectively.
DC9305 PF-CBP1(PF-06670910) hydrochloride PF-CBP1 is potent and highly-selective inhibitor of the bromodomain of CREB binding protein (CBP BRD) that down regulates targets of CBP in macrophages primary neurons.
DC7850 OF-1 OF-1 is a potent inhibitor of BRPF1B and BRPF2 bromodomain with Kd of 100 nM and 500 nM, respectively.
DC9758 NI-57 NI-57 is a potent inhibitor of the bromodomains of BRPF proteins that binds to BRPF1B, BRPF2, and BRPF3 with Kd values of 31, 108, and 408 nM, respectively, as determined by isothermal titration calorimetry.
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