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Takinib

(Synonyms: EDHS-206)
30 Cited Publications
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Based on 30 publication(s) in Google Scholar

Takinib (EDHS-206) is an orally active and selective TAK1 inhibitor (IC50=9.5 nM), more than 1.5 log more potent than the second and third ranked targets, IRAK4 (120 nM) and IRAK1 (390 nM), respectively. Takinib is an inhibitor of autophosphorylated TAK1 that non-competitively binds within the ATP binding pocket. Takinib induces apoptosis following TNFα stimulation in cell models of rheumatoid arthritis and metastatic breast cancer. Takinib is also a P. falciparum protein kinase 9 (PfPK9) inhibitor (KD(app) of 0.46 μM).

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  • Pureza: 99.48%
  • No. CAS: 1111556-37-6
  • Fòrmula: C18H18N4O2
  • Peso molecular:322.36
  • Almacenamiento:
    Powder   -20°C, 3 years , 4°C, 2 years ; In solvent   -80°C, 1 year , -20°C, 6 months
  • Takinib Chemical Structure
    Takinib Chemical Structure
  • Experimental Validation Results for Takinib
  • Experimental Validation Results for Takinib
  • Experimental Validation Results for Takinib
  • Experimental Validation Results for Takinib
  • Experimental Validation Results for Takinib
  • Experimental Validation Results for Takinib
No. CAS: 1111556-37-6
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  • Takinib Chemical Structure
    Takinib Chemical Structure
    1/16
  • 1/16

    Takinib purchased from MedChemExpress. Usage Cited in: J Adv Res. 2024 Dec 9:S2090-1232(24)00565-4. [Abstract]

    Customer Validation
     The activity of ALP in MCOBs following a 14-day exposure to OM with or without Takinib.

  • 1/16

    Takinib purchased from MedChemExpress. Usage Cited in: J Adv Res. 2024 Dec 9:S2090-1232(24)00565-4. [Abstract]

    Customer Validation
     ARS staining of calcium deposition in MCOBs following a 21-day exposure to OM with or without Takinib (1 × magnification). Quantitative assessment of the calcium deposition.

  • 1/16

    Takinib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Jun 27;15(1):5441. [Abstract]

    Customer Validation
     MPC5 cells transfected with si-OTUD5 were pretreated with 10 μM Takinib (TAK1 inhibitor) for 1 h before exposure to HG/PA. Levels of P-TAK1, P-ERK, P-P38, and P-JNK were detected by western blot.

  • 1/16

    Takinib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Jun 27;15(1):5441. [Abstract]

    Customer Validation
     MPC5 cells transfected with si-OTUD5 were pretreated with 10 μM Takinib (TAK1 inhibitor) for 1 h before exposure to HG/PA. Real-time qPCR showing mRNA levels of Il6 and Tnfα.

  • 1/16

    Takinib purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2024 Jun 21;15(6):438. [Abstract]

    Customer Validation
     The Caco-2 and SW480 cells were transfected with control and RGS16 siRNA for 48 h, and then treated with DMSO or Takinib for 8 h. The RGS16 and the activation of indicated protein were examined by Western blotting.

  • 1/16

    Takinib purchased from MedChemExpress. Usage Cited in: Mol Biol Cell. 2018 Oct 1;29(20):2470-2480. [Abstract]

    Customer Validation
     WT and WDR62-KO cells are pre-incubated withTakinib (2 µM) for 1 h then treated with TNFα (50 ng/mL) for 15 min. JNK activation is determined by Western blotting.

  • Takinib