HS-276

CAS No. 2767422-72-8

HS-276( —— )

Catalog No. M35623 CAS No. 2767422-72-8

HS-276 is a highly selective, orally active inhibitor of TAK1 (Ki: 2.5 nM). HS-276 significantly inhibits TAK1 (IC50: 8.25 nM), CLK2 (IC50: 29 nM), GCK (IC50: 22 nM), ULK2 (IC50: 63 nM), MAP4K5 (IC50. HS-276 can be used to study rheumatoid arthritis (RA).

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
1 mL x 10 mM in DMSO 164 In Stock
5MG 140 In Stock
10MG 219 In Stock
25MG 430 In Stock
50MG 676 In Stock
100MG 1042 In Stock
200MG 1404 In Stock
500MG Get Quote In Stock
1G Get Quote In Stock

Biological Information

  • Product Name
    HS-276
  • Note
    Research use only, not for human use.
  • Brief Description
    HS-276 is a highly selective, orally active inhibitor of TAK1 (Ki: 2.5 nM). HS-276 significantly inhibits TAK1 (IC50: 8.25 nM), CLK2 (IC50: 29 nM), GCK (IC50: 22 nM), ULK2 (IC50: 63 nM), MAP4K5 (IC50. HS-276 can be used to study rheumatoid arthritis (RA).
  • 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.
  • 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.
  • 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.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%.
  • Synonyms
    ——
  • Pathway
    MAPK/ERK Signaling
  • Target
    p38 MAPK
  • Recptor
    MAPK
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2767422-72-8
  • Formula Weight
    419.52
  • Molecular Formula
    C24H29N5O2
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 50 mg/mL (119.18 mM; ultrasonic and warming and adjust pH to 2 with HCl and heat to 80°C )
  • SMILES
    C(CC)N1C=2C(N=C1NC(=O)C3=CC(C(N)=O)=CC=C3)=CC=C(CN4CCCCC4)C2
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

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.?
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