1. Apoptosis
  2. RIP kinase
  3. GSK2982772

GSK2982772 

Cat. No.: HY-101760 Purity: >98.0%
Handling Instructions

GSK2982772 is a potent and ATP competitive RIP1 inhibitor with an IC50 of 16 nM.

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

GSK2982772 Chemical Structure

GSK2982772 Chemical Structure

CAS No. : 1622848-92-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 149 In-stock
Estimated Time of Arrival: December 31
1 mg USD 80 In-stock
Estimated Time of Arrival: December 31
5 mg USD 180 In-stock
Estimated Time of Arrival: December 31
10 mg USD 280 In-stock
Estimated Time of Arrival: December 31
50 mg USD 840 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1520 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Description

GSK2982772 is a potent and ATP competitive RIP1 inhibitor with an IC50 of 16 nM.

IC50 & Target

IC50: 16 nM (human RIP1 FP), 20 nM (monkey RIP1 FP), 2 μM (rat RIP1 FP), 2.5 μM (mouse RIP1 FP)[1]

In Vitro

GSK2982772 shows more than 1,000-fold selectivity for ERK5 over a panel of over 339 kinases at 10 μM. In stimulated cellular systems,GSK2982772 is also able to reduce spontaneous production of cytokines (IL-1β and IL-6) in a concentration-dependent fashion from ulcerative colitis explant tissue in overnight incubations. GSK2982772 produces a weak concentration dependent inhibition of hERG in human embryonic kidney (HEK-293) cells, with an estimated IC50 of 195 μM, and also shows a weak activation of the human Pregnane X receptor (hPXR) with an EC50 of 13 μM[1].

In Vivo

GSK2982772 is dosed orally 15 min prior to TNF and shows 68, 80, and 87% protection from temperature loss over 6 h, at doses of 3, 10, and 50 mg/kg, respectively. In the corresponding TNF/zVAD model, GSK2982772 shows 13, 63, and 93% protection from temperature loss over 3 h. GSK2982772 displays a good free fraction in blood in rats (4.2%), dogs (11%), cynomolgus monkeys (11%), and humans (7.4%). The inhibitor has a good pharmacokinetic profile across both rats and monkeys. GSK2982772 distributes into a range of tissues including the colon, liver, kidney, and heart at concentrations comparable to those of blood. However, GSK2982772 has low brain penetration in rat (4%) despite possessing good cell permeability (21×10-6 cm/s)[1].

Clinical Trial
Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (264.97 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6497 mL 13.2485 mL 26.4971 mL
5 mM 0.5299 mL 2.6497 mL 5.2994 mL
10 mM 0.2650 mL 1.3249 mL 2.6497 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[1]

Mice: A total of 7 mice per dose group are orally predosed with saline or GSK2982772 at doses of 3, 10, and 50 mg/kg 15 min before i.v. administration of mouse TNF (30 μg/ mouse). Temperature loss in the mice is measured by a rectal probe. The study is terminated after 6 h when the control group lost 7 °C[1].

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

References
Molecular Weight

377.40

Formula

C₂₀H₁₉N₅O₃

CAS No.

1622848-92-3

SMILES

O=C(C1=NC(CC2=CC=CC=C2)=NN1)N[[email protected]]3COC4=CC=CC=C4N(C)C3=O

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
GSK2982772
Cat. No.:
HY-101760
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GSK2982772

Cat. No.: HY-101760