1. Epigenetics
  2. Epigenetic Reader Domain
  3. GSK973

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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5 mg USD 370 In-stock
10 mg USD 595 In-stock
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Based on 1 publication(s) in Google Scholar

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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].

MedChemExpress (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.
Appearance

Solid

Color

Off-white to light yellow

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (304.55 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4364 mL 12.1820 mL 24.3641 mL
5 mM 0.4873 mL 2.4364 mL 4.8728 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

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g

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4364 mL 12.1820 mL 24.3641 mL 60.9102 mL
5 mM 0.4873 mL 2.4364 mL 4.8728 mL 12.1820 mL
10 mM 0.2436 mL 1.2182 mL 2.4364 mL 6.0910 mL
15 mM 0.1624 mL 0.8121 mL 1.6243 mL 4.0607 mL
20 mM 0.1218 mL 0.6091 mL 1.2182 mL 3.0455 mL
25 mM 0.0975 mL 0.4873 mL 0.9746 mL 2.4364 mL
30 mM 0.0812 mL 0.4061 mL 0.8121 mL 2.0303 mL
40 mM 0.0609 mL 0.3046 mL 0.6091 mL 1.5228 mL
50 mM 0.0487 mL 0.2436 mL 0.4873 mL 1.2182 mL
60 mM 0.0406 mL 0.2030 mL 0.4061 mL 1.0152 mL
80 mM 0.0305 mL 0.1523 mL 0.3046 mL 0.7614 mL
100 mM 0.0244 mL 0.1218 mL 0.2436 mL 0.6091 mL
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GSK973 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
GSK973
Cat. No.:
HY-138563
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