1. MAPK/ERK Pathway
  2. p38 MAPK
  3. Talmapimod hydrochloride

Talmapimod hydrochloride (Synonyms: SCIO-469 hydrochloride)

Cat. No.: HY-10406A
Handling Instructions

Talmapimod (SCIO-469) hydrochloride is an orally active, selective, and ATP-competitive p38α inhibitor with an IC50 of 9 nM. Talmapimod hydrochloride shows about 10-fold selectivity over p38β, and at least 2000-fold selectivity over a panel of 20 other kinases, including other MAPKs.

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Talmapimod hydrochloride Chemical Structure

Talmapimod hydrochloride Chemical Structure

CAS No. : 309915-12-6

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Description

Talmapimod (SCIO-469) hydrochloride is an orally active, selective, and ATP-competitive p38α inhibitor with an IC50 of 9 nM. Talmapimod hydrochloride shows about 10-fold selectivity over p38β, and at least 2000-fold selectivity over a panel of 20 other kinases, including other MAPKs[1][2][3].

IC50 & Target[1]

p38α

9 nM (IC50)

p38β

90 nM (IC50)

In Vitro

Talmapimod (SCIO-469) hydrochloride (100-200 nM; 1 hour) inhibits phosphorylation of p38 MAPK in MM cells[1].
Talmapimod hydrochloride inhibits LPS-induced TNF-a production in human whole blood[2].
Talmapimod hydrochloride decreases constitutive p38alpha MAPK phosphorylation of both 5T2MM and 5T33MM cells[3].

Western Blot Analysis[1]

Cell Line: MM.1S, U266, RPMI8226, MM.1R, and RPMI-Dox40 cell lines
Concentration: 100, 200 nM
Incubation Time: 1 hour
Result: Strongly inhibits phosphorylation of p38 MAPK.
In Vivo

Talmapimod hydrochloride (10-90 mg/kg; P.o.; twice daily orally for 14 days) dose-dependently reduced tumor growth and also dose-dependently reduced weight of the palpable tumors at termination[4].

Animal Model: Six-week-old male triple immune-deficient BNX mice (RPMI-8226 MM palpable tumors)[4]
Dosage: 10, 30, 90 mg/kg
Administration: P.o.; twice daily orally for 14 days
Result: Dose-dependently reduced tumor growth.
Molecular Weight

549.46

Formula

C₂₇H₃₁Cl₂FN₄O₃

CAS No.

309915-12-6

SMILES

O=C(N(C)C)C(C1=CN(C)C2=C1C=C(C(N3[[email protected]](C)CN(CC4=CC=C(F)C=C4)[[email protected]@H](C)C3)=O)C(Cl)=C2)=O.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

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Keywords:

TalmapimodSCIO-469SCIO469SCIO 469p38 MAPKmultiplemyelomacellsHsp27tumorcytotoxicityphosphorylationInhibitorinhibitorinhibit

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Talmapimod hydrochloride
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