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 | |
| 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 |
| Molecular Formula | C24H29N5O2 |
|---|---|
| Molecular Weight | 419.52 |