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Merck
CN

SML3629

HS-276

≥98% (HPLC)

Synonym(s):

HS 276, HS276, N1-[6-(1-Piperidinylmethyl)-1-propyl-1H-benzimidazol-2-yl]-1,3-benzenedicarboxamide

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About This Item

Empirical Formula (Hill Notation):
C24H29N5O2
CAS Number:
Molecular Weight:
419.52
UNSPSC Code:
12352200
NACRES:
NA.77
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InChI key

NPEMHKSMWPZEOV-UHFFFAOYSA-N

SMILES string

O=C(C1=CC=CC(C(NC2=NC3=C(N2CCC)C=C(CN4CCCCC4)C=C3)=O)=C1)N

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear (Warmed)

storage temp.

2-8°C

Quality Level

Biochem/physiol Actions

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) that 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.).
Orally available, potent and selective TGF-β-activated kinase-1 (TAK-1; TAK1) inhibitor.

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Regulatory Information

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Scott Scarneo et al.
ACS chemical biology, 17(3), 536-544 (2022-03-03)
Selective targeting of TNF in inflammatory diseases such as rheumatoid arthritis (RA) has provided great therapeutic benefit to many patients with chronic RA. Although these therapies show initially high response rates, their therapeutic benefit is limited over the lifetime of

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