1. Immunology/Inflammation Apoptosis Stem Cell/Wnt Cell Cycle/DNA Damage
  2. IRAK TNF Receptor Casein Kinase Interleukin Related
  3. HS-276 hydrochloride

HS-276 hydrochloride is an orally active, potent and highly selective TAK1 inhibitor, with a Ki of 2.5 nM. HS-276 hydrochloride 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 hydrochloride reduces the expression of TNF, IL-6, and IL-1β. HS-276 hydrochloride can be used for rheumatoid arthritis (RA) research.

For research use only. We do not sell to patients.

HS-276 hydrochloride

HS-276 hydrochloride Chemical Structure

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Description

HS-276 hydrochloride is an orally active, potent and highly selective TAK1 inhibitor, with a Ki of 2.5 nM. HS-276 hydrochloride 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 hydrochloride reduces the expression of TNF, IL-6, and IL-1β. HS-276 hydrochloride can be used for rheumatoid arthritis (RA) research[1].

IC50 & Target[1]

IRAK1

264 nM (IC50)

IRAK4

2500 nM (IC50)

IL-6

201 nM (IC50)

IL-1β

234 nM (IC50)

In Vitro

HS-276 hydrochloride reduces expression of TNF, IL-6, and IL-1β in a dose-dependent manner, with IC50 values of 138, 201, and 234 nM, respectively[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

HS-276 (CIA mouse model of inflammatory arthritis, 50 mg/kg, IP, daily for 6 days) hydrochloride 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, p.o., once) hydrochloride shows excellent bioavailability in mice with a Cmax of 3.68 μM and %F of 98.1%[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

455.98

Formula

C24H30ClN5O2

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
HS-276 hydrochloride
Cat. No.:
HY-147141A
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