HS-276
- CAS No.
- 2767422-72-8
- Chemical Name:
- HS-276
- Synonyms
- HS-276;HS-276, 10 mM in DMSO;N-(6-(Piperidin-1-ylmethyl)-1-propyl-1H-benzo[d]imidazol-2-yl)isophthalamide;1,3-Benzenedicarboxamide, N1-[6-(1-piperidinylmethyl)-1-propyl-1H-benzimidazol-2-yl]-
- CBNumber:
- CB710754602
- Molecular Formula:
- C24H29N5O2
- Molecular Weight:
- 419.52
- MDL Number:
- MOL File:
- 2767422-72-8.mol
| Density | 1.28±0.1 g/cm3(Predicted) |
|---|---|
| storage temp. | Store at -20°C |
| solubility | DMSO : 50 mg/mL (119.18 mM; ultrasonic and warming and adjust pH to 2 with HCl and heat to 80°C) |
| pka | 12.32±0.43(Predicted) |
| form | Solid |
| color | Off-white to light yellow |
| FDA UNII | WC3BRW6EWP |
| UNSPSC Code | 12352200 |
| NACRES | NA.77 |
HS-276 Chemical Properties,Uses,Production
Uses
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].
Biological Activity
HS-276 is an orally active, potent and selective TGF-β-activated kinase-1 (TAK-1; TAK1) inhibitor (Ki = 2.5 nM; IC50 = 8.25 nM) th at significantly reduced cytokines production in THP-1 human macrophages upon LPS/IFNγ treatment (IC50 = 138 nM/TNF, 201 nM/IL-6, and 234 nM/IL-1β). HS-276 effectively attenuates arthritic-like symptoms in the CIA mouse rheumatoid arthritis (RA) model (10-30 mg/kg/d p.o. or 25 mg/kg/d i.p.).
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].
IC 50
IRAK1: 264 nM (IC50); IRAK4: 2500 nM (IC50)
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. DOI:10.1021/acschembio.1c00788
HS-276 Preparation Products And Raw materials
Raw materials
Preparation Products
HS-276 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 32239 | 58 |
| Nantong HI-FUTURE Biology Co., Ltd. | +undefined18051384581 | sales@chemhifuture.com | China | 3135 | 58 |
| Aladdin Scientific | tp@aladdinsci.com | United States | 52924 | 58 | |
| Nantong Hi-Future Biotechnology Co., Ltd | 18051384581 | sales@chemhifuture.com | China | 3018 | 58 |
| Bide Pharmatech Ltd. | 400-1647117 13681763483 | product02@bidepharm.com | China | 62072 | 58 |
| TargetMol Chemicals Inc. | 4008200310 | marketing@tsbiochem.com | China | 24739 | 58 |
| Suzhou Zhixin Biotechnology Co., Ltd. | 0512-65118909 15162312715 | sales@szzxbio.com | China | 2972 | 58 |
| Shanghai Tachizaki Biomedical Research Center | 18014399201 | sales@chemlab-tachizaki.com | China | 2672 | 58 |
| Shanghai Yifei Biotechnology Co. , Ltd. | 021-65675885 18964387627 | customer_service@efebio.com | China | 11973 | 58 |
| RD International Technology Co., Limited | 18024082417 | market@ubiochem.com | China | 9835 | 58 |
