GSK2982772

Catalog No.S8484 Batch:S848401

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Technical Data

Formula

C20H19N5O3
Molecular Weight 377.40 CAS No. 1622848-92-3
Solubility (25°C)* In vitro DMSO 75 mg/mL (198.72 mM)
Ethanol 30 mg/mL (79.49 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description GSK2982772 is an ATP competitive receptor-interacting protein-1 (RIP1) kinase (RIPK1) inhibitor with the IC50 value of 16 nM. It has exquisite kinase specificity and excellent activity in blocking many TNF-dependent cellular responses.
Targets
human RIP1 [1]
(Cell-free assay)
16 nM
In vitro

GSK2982772 has excellent activity in both RIP1 cellular systems, preventing TNF induced necrotic cell death, and an ulcerative colitis explant assay blocking spontaneous cytokine release[1].
In vivo

GSK2982772 exhibits approximately equivalent RIP1 FP potency against human and monkey RIP1 but was significantly less potent against nonprimate RIP1. 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, it has low brain penetration in rat (4%) despite possessing good cell permeability, which is likely due to active extrusion of GSK2982772 from the brain via the efflux drug transporter. It is predicted that GSK2982772 has high bioavailability, moderate to low clearance with a moderate volume, and a terminal half-life in the order of 12 h[1].

Protocol (from reference)

Animal Study:

[1]
  • Animal Models

    TNF/zVAD mouse model

  • Dosages

    3, 10, and 50 mg/kg

  • Administration

    oral administration

Selleck's GSK2982772 has been cited by 4 publications

Necrostatin-1 Prevents Ferroptosis in a RIPK1- and IDO-Independent Manner in Hepatocellular Carcinoma [ Antioxidants (Basel), 2021, 10(9)1347] PubMed: 34572979
Pleiotropic, non-cell death-associated effects of inhibitors of receptor-interacting protein kinase 1 in the heart [ Mol Cell Biochem, 2021, 10.1007/s11010-021-04136-y] PubMed: 33811579
Inflammatory signals induce MUC16 expression in ovarian cancer cells via NF-κB activation [ Exp Ther Med, 2021, 21(2):163] PubMed: 33456530
Targeted enhancement of the therapeutic window of L19-TNF by transient and selective inhibition of RIPK1-signaling cascade. [ Oncotarget, 2019, 10(62):6678-6690] PubMed: 31803362

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.