GSK481 free base · Synonyms: GSK'481

GSK481 is a potent inhibitor of Receptor-interacting serine/threonine-protein kinase 1 exhibiting a remarkable specificity over >450 other kinases.

For research use only. Not for human or veterinary use.

Target RIP kinase

Research area Inflammation/Immunology

Purity >98% Stock Inquire

Data Sheet SDS COA

GSK481 structure

CAS No.: 1622849-58-4

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
100 mg	USD 875.00	BP-02346-100mg	In stock	Get quote
200 mg	USD 1,185.00	BP-02346-200mg	In stock	Get quote
500 mg	USD 1,450.00	BP-02346-500mg	In stock	Get quote
1 g	USD 2,150.00	BP-02346-1g	In stock	Get quote
2 g	Inquire	BP-02346-2g	In stock	Inquire
5 g	Inquire	BP-02346-5g	In stock	Inquire

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Description

GSK481 is a potent inhibitor of Receptor-interacting serine/threonine-protein kinase 1 (RIPK1 or RIP1; IC50 value 2.8 nM for inhibition of S166 phosphorylation of hWT RIP1) exhibiting a remarkable specificity over >450 other kinases. GSK'481 protects against TNF-induced inflammation and lethal shock.

Biological activity

GSK481 is a highly effective, selective and specific RIPK1 inhibitor with an IC50 value of 1.3 nM, which can inhibit the phosphorylation of Ser166 in wild-type human RIPK1 (IC50 value of 2.8 nM). The IC50 value of GSK481 against U937 cells was 10 nM.

Identifiers

SMILES: CN1C2=CC=CC=C2OC[C@H](NC(=O)C2=NOC(CC3=CC=CC=C3)=C2)C1=O
InChIKey: KNOUWGGQMADIBV-KRWDZBQOSA-N

Specifications

MW (average): 377.3933
Formula: C₂₁H₁₉N₃O₄
CAS No.: 1622849-58-4
Physical state: Solid
Color: Light brown to brown
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

References

[1]. Harris PA et al. DNA-Encoded Library Screening Identifies Benzo[b][1,4]oxazepin-4-ones as Highly Potent and Monoselective Receptor Interacting Protein 1 Kinase Inhibitors. J Med Chem, 2016 Mar 10, 59(5):2163-78.

[2]. Lee HL, et al. Simultaneous flow cytometric immunophenotyping of necroptosis, apoptosis and RIP1-dependent apoptosis. Methods. 2018 Feb 1;134-135:56-66.

Same target

Search RIP kinase

Same research area

Search Inflammation/Immunology