Home Cart Sign in  
Chemical Structure| 1111556-37-6 Chemical Structure| 1111556-37-6

Structure of Takinib
CAS No.: 1111556-37-6

Chemical Structure| 1111556-37-6

*Storage: {[sel_prStorage]}

*Shipping: {[sel_prShipping]}

,{[proInfo.pro_purity]}

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 !

{[proInfo.pro_purity]}
Cat. No.: {[proInfo.prAm]} Purity: {[proInfo.pro_purity]}

Change View

Size Price VIP Price

US Stock

Global Stock

In Stock
{[ item.pr_size ]} Inquiry {[ getRatePrice(item.pr_usd,item.pr_rate,item.mem_rate,item.pr_is_large_size_no_price, item.vip_usd) ]}

US Stock: ship in 0-1 business day
Global Stock: ship in 5-7 days

  • {[ item.pr_size ]}

In Stock

- +

Please Login or Create an Account to: See VIP prices and availability

US Stock: ship in 0-1 business day
Global Stock: ship in 2 weeks

  • 1-2 Day Shipping
  • High Quality
  • Technical Support
Product Citations

Alternative Products

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

Related Pathways of Takinib

MAPK
pyroptosis
TLR

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
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 References
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

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.10mL

0.62mL

0.31mL

15.51mL

3.10mL

1.55mL

31.02mL

6.20mL

3.10mL

References

 

Historical Records

Categories