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GSK872 HCl（1346546-69-7 free base）

Catalog No. T4074L CAS 2703752-81-0

Synonyms: GSK2399872A

GSK872 HCl（1346546-69-7 free base） (GSK2399872A) is an effective and specific RIP3 kinase inhibitor. It binds RIP3 kinase domain with high affinity (IC50: 1.8 nM) and inhibits kinase activity (IC50: 1.3 nM).

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GSK872 HCl（1346546-69-7 free base） Chemical Structure

GSK872 HCl（1346546-69-7 free base）, CAS 2703752-81-0

Pack Size	Availability	Price/USD
1 mg	In stock	$ 31.00
2 mg	In stock	$ 44.00
5 mg	In stock	$ 72.00
10 mg	In stock	$ 122.00
25 mg	In stock	$ 261.00
50 mg	In stock	$ 477.00
100 mg	In stock	$ 698.00
1 mL * 10 mM (in DMSO)	In stock	$ 79.00

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Purity: 99.82%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	GSK872 HCl（1346546-69-7 free base） (GSK2399872A) is an effective and specific RIP3 kinase inhibitor. It binds RIP3 kinase domain with high affinity (IC50: 1.8 nM) and inhibits kinase activity (IC50: 1.3 nM).
Targets&IC50	RIP3K:1.8 nM
In vitro	GSK872 (1 μM) has no inhibition for most of 300 human protein kinases tested. It fails to inhibit RIP1 kinase. In HT-29 cells, GSK872 concentration-dependently blocks TNF-induced necroptosis. In cell-based assays, there is a 100- to 1000-fold shift in the IC50 compared to the cell-free biochemical assays. GSK872 inhibits DAI- or TLR3-induced (RIP1-independent) death. It induces caspase activation and then induces apoptotic cell death[1].
In vivo	In compared with no treatment after ischemic injury in vivo, GSK872 can significantly reduce HIF-1α expression [3].

Synonyms	GSK2399872A
Molecular Weight	419.94
Formula	C19H18ClN3O2S2
CAS No.	2703752-81-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (260.76 mM)

References and Literature

1. Mandal P, et al. RIP3 induces apoptosis independent of pronecrotic kinase activity. Mol Cell. 2014, 56(4):481-95. 2. Kaiser WJ, et al. Toll-like receptor 3-mediated necrosis via TRIF, RIP3, and MLKL. J Biol Chem. 2013 Oct 25;288(43):31268-79. 3. Yang XS, et al. Hypoxia-inducible factor-1 alpha is involved in RIP-induced necroptosis caused by in vitro and in vivo ischemic brain injury.Sci Rep. 2017 Jul 19;7(1):5818.

Related compound libraries

This product is contained In the following compound libraries：

Kinase Inhibitor Library Inhibitor Library Bioactive Compounds Library Max Anti-Breast Cancer Compound Library Pyroptosis Compound Library Anti-Cancer Compound Library NF-κB Signaling Compound Library Anti-Prostate Cancer Compound Library Apoptosis Compound Library Immunology/Inflammation Compound Library

Related Products

Related compounds with same targets

RIPK2-IN-3 RIPK3-IN-4 GSK2983559 free acid Necrostatin 2 racemate RIP1 kinase inhibitor 5 Necrostatin-34 GSK2982772 Necrostatin-5

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Keywords

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