2767422-72-8

2767422-72-8 structure

Name: HS-276
Chemical Name: HS-276
CAS Number: 2767422-72-8
Molecular Formula: C₂₄H₂₉N₅O₂
Molecular Weight: 419.52
Catalog: Signaling Pathways Immunology/Inflammation IRAK
Create Date: 2022-07-30 17:20:10
Modify Date: 2024-01-08 19:04:34
HS-276 is an orally active, potent and highly selective TAK1 inhibitor, with a Ki of 2.5 nM. HS-276 shows significant inhibition of TAK1, CLK2, GCK, ULK2, MAP4K5, IRAK1, NUAK, CSNK1G2, CAMKKβ-1, and MLK1, with IC50 values of 8.25, 29, 33, 63, 125, 264, 270, 810, 1280, and 5585 nM, respectively. HS-276 can be used for rheumatoid arthritis (RA) research[1].

Name	HS-276

Description	HS-276 is an orally active, potent and highly selective TAK1 inhibitor, with a Ki of 2.5 nM. HS-276 shows significant inhibition of TAK1, CLK2, GCK, ULK2, MAP4K5, IRAK1, NUAK, CSNK1G2, CAMKKβ-1, and MLK1, with IC50 values of 8.25, 29, 33, 63, 125, 264, 270, 810, 1280, and 5585 nM, respectively. HS-276 can be used for rheumatoid arthritis (RA) research[1].
Related Catalog	Signaling Pathways >> Immunology/Inflammation >> IRAK Research Areas >> Inflammation/Immunology Signaling Pathways >> Protein Tyrosine Kinase/RTK >> IRAK
Target	IRAK1:264 nM (IC50) IRAK4:2500 nM (IC50)
In Vitro	HS-276 reduces expression of TNF, IL-6, and IL-1β in a dose-dependent manner, with IC50 values of 138, 201, and 234 nM, respectively[1].
In Vivo	HS-276 (CIA mouse model of inflammatory arthritis, 50 mg/kg, IP, daily for 6 days) reduces inflammation, pannus, cartilage damage (CD), bone resorption (BR), and periosteal bone formation (PBF) histological manifestations[1]. HS-276 (CD-1 mice, 30 mg/kg, Oral gavage, once) shows excellent bioavailability in mice with a Cmax of 3.68 μM and %F of 98.1%[1].
References	[1]. Scarneo S, et al. Development and Efficacy of an Orally Bioavailable Selective TAK1 Inhibitor for the Treatment of Inflammatory Arthritis. ACS Chem Biol. 2022 Mar 18;17(3):536-544.

Molecular Formula	C₂₄H₂₉N₅O₂
Molecular Weight	419.52