Takinib

Research use only, not for human use.

Takinib is a potent, selective TAK1 inhibitor with IC50 of 9.5 nM, selectively induces apoptosis following TNF-a stimulation.

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.

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-231Concentration: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.

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.

Takinib | EDHS-206 | EDHS 206 | EDHS206

NF-κB

TAK1

TAK1

Inflammation/Immunology

——

1111556-37-6

322.368

C18H18N4O2

>98% (HPLC)

DMSO: 6.8 mg/mL （ < 1 mg/ml refers to the product slightly soluble or insoluble )

O=C(C1=CC=CC(C(NC2=NC3=CC=CC=C3N2CCC)=O)=C1)N

1,3-Benzenedicarboxamide, N1-(1-propyl-1H-benzimidazol-2-yl)-

(-20℃)

With Ice Pack

≥ 2 years