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Talmapimod

Catalog No. T12871 CAS 309913-83-5

Synonyms: SCIO-469

Talmapimod (SCIO-469) is an selective, orally active, and ATP-competitive p38α inhibitor with IC50 of 9 nM and 90 nM for p38α and p38β, respectively. Talmapimod exhibits at least 2000-fold selectivity over a panel of 20 kinases, including other MAPKs.

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Talmapimod, CAS 309913-83-5

Pack Size	Availability	Price/USD
1 mg	In stock	$ 48.00
2 mg	In stock	$ 70.00
5 mg	In stock	$ 117.00
10 mg	In stock	$ 187.00
25 mg	In stock	$ 397.00
50 mg	In stock	$ 589.00
100 mg	In stock	$ 843.00
1 mL * 10 mM (in DMSO)	In stock	$ 133.00

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Purity: 100%

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Description	Talmapimod (SCIO-469) is an selective, orally active, and ATP-competitive p38α inhibitor with IC50 of 9 nM and 90 nM for p38α and p38β, respectively. Talmapimod exhibits at least 2000-fold selectivity over a panel of 20 kinases, including other MAPKs.
Targets&IC50	p38β:90 nM, p38α:9 nM
In vitro	phosphorylation of p38 MAPK inhibited by Talmapimod (100-200 nM; 1 hour) in MM cells[1].In human whole blood, LPS-induced TNF-a production inhibited by Talmapimod [2]. Talmapimod decreases constitutive p38alpha MAPK phosphorylation of both 5T2MM and 5T33MM cells[3].
In vivo	Targeting p38α MAPK with Talmapimod (SCIO-469) decreases myeloma burden,and preventing the development of myeloma bone disease[2]. In 5T2MM and 5T33MM models，Talmapimod inhibits the growth of multiple myeloma and prevents bone diseases[3]. Talmapimod (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].

Synonyms	SCIO-469
Molecular Weight	513
Formula	C27H30ClFN4O3
CAS No.	309913-83-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 95 mg/mL (185.19 mM)

References and Literature

1. Hideshima T et al. p38 MAPK inhibition enhances PS-341 (bortezomib)-induced cytotoxicity against multiple myeloma cells. Oncogene. 2004 Nov 18, 23(54), 8766-76. 2. Navas T, et al. Inhibition of p38alpha MAPK disrupts the pathological loop of proinflammatory factor production in the myelodysplastic syndrome bone marrow microenvironment. Leuk Lymphoma. 2008 Oct;49(10):1963-75. 3. Vanderkerken K et al. Inhibition of p38alpha mitogen-activated protein kinase prevents the development of osteolytic bone disease,reduces tumor burden, and increases survival in murine models of multiple myeloma. Cancer Res. 2007 May 15;67(10):4572-7. 4. Medicherla S, et al. p38alpha-selective MAP kinase inhibitor reduces tumor growth in mouse xenograft models of multiple myeloma. Anticancer Res. 2008 Nov-Dec;28(6A):3827-33.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Inhibitor Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library Bioactive Compounds Library Max Kinase Inhibitor Library Orally Active Compound Library Cytoskeletal Signaling Pathway Compound Library Anti-Ovarian Cancer Compound Library

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Keywords

Talmapimod 309913-83-5 MAPK p38 MAPK cytotoxicity multiple inhibit tumor SCIO469 cells SCIO-469 Hsp27 Inhibitor phosphorylation SCIO 469 myeloma inhibitor

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