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Chemical Structure| 1111556-37-6 Chemical Structure| 1111556-37-6
Chemical Structure| 1111556-37-6

*Storage: Sealed in dry,2-8°C.

Takinib

CAS No.: 1111556-37-6

Takinib (EDHS-206) is an orally active and selective TAK1 inhibitor with an IC50 of 9.5 nM, significantly more potent than its next closest targets, IRAK4 (120 nM) and IRAK1 (390 nM). It non-competitively binds within the ATP binding pocket, induces apoptosis following TNFα stimulation in cell models of rheumatoid arthritis and metastatic breast cancer, and inhibits PfPK9 with a KD(app) of 0.46 μM.

Synonyms: EDHS-206

4.5 *For Research Use Only !

Cat. No.: A949172 Purity: 98%

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Product Details of [ Takinib ]

CAS No. :1111556-37-6
Formula : C18H18N4O2
M.W : 322.36
SMILES Code : O=C(C1=CC=CC(C(N)=O)=C1)NC2=NC3=CC=CC=C3N2CCC
Synonyms :
EDHS-206
MDL No. :MFCD11822633

Safety of [ Takinib ]

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description Reference
RA-FLS 1 μM 24 h HS-243 showed robust inhibition of IRAK-4 PMC7008364
MPC-11 1 μM and 0.2 μM 72 hours To evaluate the inhibitory effect of Takinib on MPC-11 cell growth, the results showed that Takinib had a GI50 value of 8.5 μM against MPC-11 cells. PMC10809330
HEK293 cells 500 μM To screen for small molecules that bind to PfPK9, Takinib was identified as one of the compounds that bind to PfPK9. PMC6430656
P. falciparum-infected erythrocytes 30 μM 24 hours To evaluate the effect of Takinib on K63-linked ubiquitination levels in P. falciparum-infected erythrocytes, results showed that Takinib significantly reduced K63-linked ubiquitination levels. PMC6430656

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description Reference
Rats Subarachnoid hemorrhage model Intracerebroventricular 0.9 mM Single dose at 30 min post SAH insults Takinib treatment significantly improved neurological scores, reduced neuronal apoptosis, and ameliorated brain edema. PMC10682771
MRL/MpJ mice Autoimmune pancreatitis model Oral gavage 25, 50, or 75 mg/kg 5 consecutive days per week for 4 weeks To evaluate the efficacy of Takinib in autoimmune pancreatitis, results showed Takinib was ineffective PMC11591683
NSG mice KMH2 xenograft model Oral 50 mg/kg/d Once daily for 17 days Takinib significantly slowed tumor growth in the KMH2 xenograft mouse model, indicating its therapeutic potential in vivo for A20 mutant HL. PMC7682429

Protocol

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5 mM

10 mM

3.10mL

0.62mL

0.31mL

15.51mL

3.10mL

1.55mL

31.02mL

6.20mL

3.10mL

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