1. Epigenetics
  2. Epigenetic Reader Domain
  3. GSK973

GSK973 

Cat. No.: HY-138563
Handling Instructions

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).

For research use only. We do not sell to patients.

GSK973 Chemical Structure

GSK973 Chemical Structure

CAS No. : 2138473-38-6

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Description

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].

IC50 & Target[1]

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)

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

410.44

Formula

C₂₃H₂₃FN₂O₄

CAS No.
SMILES

[H][[email protected]]1([[email protected]@H]2NC(C3=CC(C(NC)=O)=C4C([[email protected]@H]([[email protected]](O4)CF)C5=CC=CC=C5)=C3)=O)[[email protected]]2([H])COC1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

GSK973GSK 973GSK-973Epigenetic Reader DomainoncologyoralsecondbromodomainsselectiveInhibitorinhibitorinhibit

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GSK973
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HY-138563
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