Takinib

SKU: orb1226972

Description

Takinib is a potent, selective TAK1 inhibitor with IC50 of 9.5 nM, selectively induces apoptosis following TNF-a stimulation; weakly inhibits IRAK4, IRAK1, GCK, CLK2, and MINK1 with IC50 of 120-430 nM against the MRC Dundee kinase panel, does not inhibit any of the MAP2Ks or MAP3Ks family members; inhibits phosphorylation of IKK, MAPK 8/9, and c-Jun, induces apoptosis in RA fibroblast-like synoviocytes and reduces IL-6 secretion, induces TNF-α-dependent cell death in rheumatoid arthritis and breast cancer cells.

Images & Validation

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Key Properties

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CAS Number	1111556-37-6
MW	322.368
Purity	>98% (HPLC)
Formula	C₁₈H₁₈N₄O₂
SMILES	O=C(C1=CC=CC(C(NC2=NC3=CC=CC=C3N2CCC)=O)=C1)N
Target	TAK1
Solubility	DMSO: 6.8 mg/mL （ < 1 mg/ml refers to the product slightly soluble or insoluble )

Bioactivity

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In Vivo

Takinib (50 mg/kg; intraperitoneally; daily from days 18-36) reduces the clinical score in type II collagen-induced arthritis (CIA) mouse model of rheumatoid arthritis. Takinib (50 mg/kg; oral gavage; daily until 17 days) slows tumor growth in the Hodgkin lymphoma xenograft NSG mice. Animal model: Male DBA/1 mice (CIA arthritis model). Dosage: 50 mg/kg. Administration: Intraperitoneally; daily from days 18-36. Result: Showed a reduction in clinical arthritic score compared to vehicle control. Animal model: Female NSG mice (8 weeks old). Dosage: 50 mg/kg. Administration: Oral gavage; daily until 17 days. Result: Slowed tumor growth and reduced tumor size/weight.

In Vitro

Takinib (10-10000 nM; 24 hours) induces apoptosis following TNF-α stimulation in MDA-MB-231 cells. Takinib (10 μM; 0-1 hours) reduces phosphorylation of IKK and p65. Takinib serves as a chemical starting point for the development of PfPK9 (KD(app) of 0.46 μM) inhibitors for malaria. Takinib (2 hours; 0.1-20 μM; human RASFs) induces phosphorylation of TAK1Thr184/187, STAT3Tyr705 and STAT3Ser727 in IL-1β-treated (10 ng/mL; 30 min) RASFs. Western blot analysis. Cell line: Breast cancer cell line MDA-MB-231. Concentration: 10 μM. Incubation time: 5, 15, 30, 60 minutes. Result: IKK and p65 were maximally phosphorylated at 15 minutes, which indicated activation of the NF-κB pathway, while p38 phosphorylation peaks at 30 minutes. Western blot analysis. Cell line: IL-1β-treated (10 ng/mL; 30 min) RASFs. Concentration: 0.1-20 μM Incubation time: 2 hours. Result: Induced phosphorylation of TAK1Thr184/187, STAT3Tyr705 and STAT3Ser727.

Storage & Handling

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Storage	Storage temperature: -20°C. Stability: ≥ 2 years
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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Takinib | EDHS-206 | EDHS 206 | EDHS206

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Gene Symbol

TAK1

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Takinib (orb1226972)

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Purity:	98.29%
CAS Number:	1111556-37-6
MW:	322.36
Formula:	C₁₈H₁₈N₄O₂

Takinib

Description

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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