Cart
sales@molnova.com
Home - Products - MAPK/ERK Signaling - p38 MAPK - HS-276

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
2MG 138 Get Quote
5MG 202 Get Quote
10MG 316 Get Quote
25MG 541 Get Quote
50MG 787 Get Quote
100MG 1062 Get Quote
500MG Get Quote Get Quote
1G Get Quote Get Quote
Get Quotation Bulk Inquiry Add to Cart

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.?
Calculator

Molecular Weight Calculator

Dilution Calculator

Molarity Calculator

molnova catalog
related products

  • p38 MAPK-IN-4

    p38 MAPK-IN-4 is a potent and selective inhibitor of p38 MAPK with IC50 of 68 nM for p38α.

  • BMS-751324

    BMS-751324 is a novel clinical prodrug of BMS-582949, which is a highly selective p38α MAPK inhibitor with IC50 of 13 nM.

  • SD-06

    SD-06 is a p38 MAP kinase inhibitor, inhibits p38α with IC50 of 170 nM and inhibits LPS-stimulated TNF-release in rats.

Sign In Join Free