| Chemical Properties | Back Directory | [Boiling point ]
550.0±50.0 °C(Predicted) | [density ]
1.36±0.1 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: 2mg/mL, clear | [form ]
Solid | [pka]
13.82±0.20(Predicted) | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Uses]
GSK973 is a highly selective, orally bioavailable inhibitor of the BD2s (second bromodomains) of the BET family, with a pIC50 of 7.8 and a pKd of 8.7 for BRD4 BD2. GSK973 displays a 1600-fold selectivity for BRD4 BD2 over BRD4 BD1. GSK973 shows good potency against BRD2 BD2, BRD3 BD2, and BRDT BD2 (pIC50=7.4~7.8; pKd=8.3~8.5)[1]. | [Biological Activity]
Orally availablepotent and selective pan-second bromodomain (BD2) inhibitor th at effectively inhibits LPS-induced MCP-1 release in human whole blood.
GSK973 is an orally availablepotent and selective pan-second bromodomain (BD2) inhibitor (BD2/BD1 pIC50 = 7.5/4.4/BRD27.8/4.5/BRD37.8/4.6/BRD47.4/4.5/BRDT) th at effectively inhibits LPS-induced MCP-1 release in human whole blood (pIC50 = 7.3; IC50 = 50 nM). | [in vivo]
GSK973 (1 mg/kg; i.v.) treatment shows the CL, CIrenal, Vss, and T1/2 are 73 mL/min/kg, 4 mL/min/kg, 2.1L/kg, and 0.6 hours, respectively[1].
GSK973 (3 mg/kg; p.o) treatment shows the Fpo of 48%[1]. | Animal Model: | Male Wistar Han Rats[1] | | Dosage: | 1 mg/kg (Pharmacokinetic Analysis) | | Administration: | I.v. | | Result: | The CL, CIrenal, Vss, and T1/2 were 73 mL/min/kg, 4 mL/min/kg, 2.1L/kg, and 0.6 hours, respectively.
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| [IC 50]
BRD4 BD2: 7.8 (pIC50); BRD2 BD2: 7.5 (pIC50); BRD3 BD2: 7.8 (pIC50); BRDT BD2: 7.4 (pIC50); BRD4 BD2: 8.7 (pKd); BRD2 BD2: 8.3 (pKd); BRD3 BD2: 8.5 (pKd); BRDT BD2: 8.3 (pKd) | [References]
[1] Preston A, et al. GSK973 Is an Inhibitor of the Second Bromodomains (BD2s) of the Bromodomain and Extra-Terminal (BET) Family. ACS Med Chem Lett. 2020;11(8):1581-1587. Published 2020 Jul 6. DOI:10.1021/acsmedchemlett.0c00247 |
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| Company Name: |
Merck KGaA
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| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
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