A TAK1 inhibitor
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HS-276

Item No. 43026

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N1-[6-(1-piperidinylmethyl)-1-propyl-1H-benzimidazol-2-yl]-1,3-benzenedicarboxamide
CAS Number
2767422-72-8
Molecular Formula
C24H29N5O2
Formula Weight
419.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/ml
SMILES
O=C(C1=CC=CC(C(NC2=NC3=C(N2CCC)C=C(CN4CCCCC4)C=C3)=O)=C1)N
InChi Code
InChI=1S/C24H29N5O2/c1-2-11-29-21-14-17(16-28-12-4-3-5-13-28)9-10-20(21)26-24(29)27-23(31)19-8-6-7-18(15-19)22(25)30/h6-10,14-15H,2-5,11-13,16H2,1H3,(H2,25,30)(H,26,27,31)
InChi Key
NPEMHKSMWPZEOV-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $94

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    10 mg

    $179

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    25 mg

    $398

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    50 mg

    $748

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    Product Description

    HS-276 is a TGF-β-activated kinase 1 (TAK1) inhibitor (IC50 = 8.25 nM).1 It is selective for TAK1 over a panel of 137 other kinases at 10 µM but does inhibit CDC-like kinase 2 (Clk2), hexokinase (HK), and unc-51-like autophagy activating kinase 2 (ULK2; IC50s = 29, 33, and 63 nM, respectively). HS-276 inhibits LPS-induced increases in secretion of TNF, IL-6, and IL-1β from THP-1 macrophages differentiated by phorbol 12-myristate 13-acetate (PMA; IC50s = 138, 201, and 234 nM, respectively). It inhibits collagen-induced increases in pannus formation, cartilage damage, bone resorption, and periosteal bone formation in a mouse model of rheumatoid arthritis when administered at a dose of 50 mg/kg twice per day.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Scarneo, S., Hughes, P., Freeze, R., et al. Development and efficacy of an orally bioavailable selective TAK1 inhibitor for the treatment of inflammatory arthritis. ACS Chem. Biol. 17(3), 536-544 (2022).