Takinib #64030

Name: Takinib
Price: 137.00 USD
Availability: InStock

Product Information

Product Usage Information

Takinib is supplied as a lyophilized powder. For a 15 mM stock, reconstitute 5 mg of powder in 1.03 mL of DMSO. Working concentrations and length of treatment can vary depending on the desired effect.

Storage

Store lyophilized at -20ºC, desiccated. In lyophilized form, the chemical is stable for 24 months. Once in solution, store at -20ºC and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Product Description

Molecular Weight	322.36 g/mol
Purity	>99%
Molecular Formula	C₁₈H₁₈N₄O₂
CAS	1111556-37-6
Solubility	Soluble in DMSO at 50 mg/mL.

Background

Takinib is a potent and selective small molecule inhibitor of TAK1, a MAP3K family protein and important moderator of cell survival and death in TNF-α signaling. Takinib preferentially binds and inhibits TAK1 (IC50 of 9.5 nM) over other targets (e.g., IRAK4: IC₅₀ of 120 nM and IRAK1: IC₅₀ of 390 nM). The inhibitor Takinib induces apoptosis following TNF-α stimulation in cell models of rheumatoid arthritis and metastatic breast cancer (1). Inhibition of TAK1 by Takinib resulted in increased cell death in several cancer cell lines, and reduced pro-inflammatory and pro-angiogenic signaling in tumor-associated macrophages, suggesting that Takinib regulation of TAK1 may be a beneficial therapeutic strategy (2). Additional evidence suggests that Takinib inhibition of cytokine production may also work along additional pathways, including the JAK/STAT pathway. In a study examining inflammation in human rheumatoid arthritis synovial fibroblasts, treatment with Takinib results in specifically reduced IL-1β-induced STAT3 phosphorylation, nuclear translocation, and DNA binding (3).

Limited Uses

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For Research Use Only. Not For Use In Diagnostic Procedures.

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