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Takinib

Background References
Product Name
Takinib
CAS No.
1111556-37-6
Chemical Name
Takinib
Synonyms
Takinib;EDHS-206;Takinib >=98% (HPLC);Takinib, 10 mM in DMSO;Takinib (EDHS-206) ，S8663;N-(1-Propyl-1H-benzo[d]imidazol-2-yl)isophthalamide;N1-(1-Propyl-1H-benzo[d]imidazol-2-yl)isophthalamide;3-N-(1-propylbenzimidazol-2-yl)benzene-1,3-dicarboxamide;1,3-Benzenedicarboxamide, N1-(1-propyl-1H-benzimidazol-2-yl)-;1-N-(1-propyl-1H-1,3-benzodiazol-2-yl)benzene-1,3-dicarboxamide
CBNumber
CB83363779
Molecular Formula
C18H18N4O2
Formula Weight
322.36
MOL File
1111556-37-6.mol
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Takinib Property

Density 
1.30±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMSO:30.0(Max Conc. mg/mL);93.06(Max Conc. mM)
form 
A solid
pka
12.13±0.43(Predicted)
color 
White to off-white
SMILES
CCCN1C2=CC=CC=C2N/C1=N\C(C3=CC(C(N)=O)=CC=C3)=O
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Safety

WGK Germany 
WGK 3
Storage Class
11 - Combustible Solids
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML2216
Product name
Takinib
Purity
≥98% (HPLC)
Packaging
5 mg
Price
$113
Updated
2026/04/30
Sigma-Aldrich
Product number
SML2216
Product name
Takinib
Purity
≥98% (HPLC)
Packaging
25 mg
Price
$454
Updated
2026/04/30
Cayman Chemical
Product number
24161
Product name
Takinib
Purity
≥98%
Packaging
1mg
Price
$36
Updated
2026/04/30
Cayman Chemical
Product number
24161
Product name
Takinib
Purity
≥98%
Packaging
5mg
Price
$95
Updated
2026/04/30
Cayman Chemical
Product number
24161
Product name
Takinib
Purity
≥98%
Packaging
10mg
Price
$169
Updated
2026/04/30
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Takinib Chemical Properties,Usage,Production

Uses

Takinib has been used as an inhibitor of transforming 28 growth factor - β-activated kinase -1 (TAK-1) in human leukemia monocytic THP-1 cells. It may be used as a TAK1 inhibitor in Jurk at cells.

Biological Activity

Takinib is a selective inhibitor of TAK1/MAP3K7 kinase, which is a member of the MAP3K family and a key regulator of cell death. It binds in the TAk1 ATPbinding pocket with an IC50 value of 9.5 nM. Takinib selectively induced apoptosis following TNF-α stimulation in rheumatoid arthritis and breast cancer.

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[4].
Takinib (50 mg/kg; oral gavage; daily until 17 days) slows tumor growth in the Hodgkin lymphoma xenograft NSG mice[5].

Animal Model:Male DBA/1 mice (CIA arthritis model)[4]
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)[5]
Dosage:50 mg/kg
Administration:Oral gavage; daily until 17 days
Result:Slowed tumor growth and reduced tumor size/weight.

IC 50

TAK1: 9.5 nM (IC50); IRAK4: 120 nM (IC50); IRAK1: 390 nM (IC50); GCK: 430 nM (IC50); CLK2: 430 nM (IC50); MINK1: 1.9 μM (IC50)

storage

Store at -20°C

Background

Takinib is a potent and selective small molecule inhibitor of TAK1, a MAP3K family protein and important moderator of cell survival and death in TNF-α signaling. Takinib preferentially binds and inhibits TAK1 over other targets. The inhibitor Takinib induces apoptosis following TNF-α stimulation in cell models of rheumatoid arthritis and metastatic breast cancer. Inhibition of TAK1 by Takinib resulted in increased cell death in several cancer cell lines, and reduced pro-inflammatory and pro-angiogenic signaling in tumor-associated macrophages, suggesting that Takinib regulation of TAK1 may be a beneficial therapeutic strategy. Additional evidence suggests that Takinib inhibition of cytokine production may also work along additional pathways, including the JAK/STAT pathway. In a study examining inflammation in human rheumatoid arthritis synovial fibroblasts, treatment with Takinib results in specifically reduced IL-1β-induced STAT3 phosphorylation, nuclear translocation, and DNA binding.

References

[1] Totzke, J. et al. (2017) Cell Chem Biol 24, 1029-1039.e7.
[2] Scarneo, S.A. et al. (2020) Oncotarget 11, 1961-1970.
[3] Panipinto, P.M. et al. (2021) Int J Mol Sci 22, 12580. doi: 10.3390/ijms222212580.

Takinib Preparation Products And Raw materials

Raw materials

Preparation Products

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Takinib Suppliers

China 79 United States 7 Global 86
Nanjing Dulai Biotechnology Co., Ltd.
Tel
025-84699383-8003;025-846993838003-8003 18013301593;18013301590
Fax
025-84699383-8003
Email
njduly@126.com
Country
China
ProdList
3293
Advantage
55
Bide Pharmatech Ltd.
Tel
400-400-164-7117 18317119277
Fax
+86-21-61629029
Email
product02@bidepharm.com
Country
China
ProdList
39999
Advantage
60
AdooQ Bioscience CHINA
Tel
025-58849295 18951903616;
Fax
025-68650336
Email
info@adooq.cn
Country
China
ProdList
2990
Advantage
60
Shanghai JiYi Biotechnology Co. Ltd.
Tel
13621943973
Fax
-
Email
sales@shjiyipharmatech.com
Country
China
ProdList
1166
Advantage
55
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696，15000506266 15000506266
Fax
+86-21-52996696
Country
China
ProdList
4827
Advantage
55
Shanghaizehan biopharma technology co., Ltd.
Tel
021-61350663 13052117465
Fax
021-61350662
Email
sales@zehanbiopharma.com
Country
China
ProdList
977
Advantage
55
Guangzhou Zhiya Chemdrugs Co.,Ltd
Tel
18122150900
Fax
QQ:2869377561
Email
sculk28@163.com
Country
China
ProdList
646
Advantage
55
BOC Sciences
Tel
16314854226
Email
info@bocsci.com
Country
United States
ProdList
9923
Advantage
65
Shanghai EFE Biological Technology Co., Ltd.
Tel
021-65675885 18964387627
Fax
021-65675885
Email
info@efebio.com
Country
China
ProdList
9803
Advantage
58
Shanghai YuanYe Biotechnology Co., Ltd.
Tel
021-61312847; 18021002903
Fax
QQ:3008007432
Email
3008007409@qq.com
Country
China
ProdList
89689
Advantage
60
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View Lastest Price from Takinib manufacturers

Career Henan Chemical Co
Product
Takinib 1111556-37-6
Price
US $1.00/g
Min. Order
1g
Purity
99.99%
Supply Ability
200kg
Release date
2019-12-23

1111556-37-6, TakinibRelated Search:

GC376 Acethydrazide

  • Takinib
  • 1-N-(1-propyl-1H-1,3-benzodiazol-2-yl)benzene-1,3-dicarboxamide
  • N-(1-Propyl-1H-benzo[d]imidazol-2-yl)isophthalamide
  • 3-N-(1-propylbenzimidazol-2-yl)benzene-1,3-dicarboxamide
  • N1-(1-Propyl-1H-benzo[d]imidazol-2-yl)isophthalamide
  • EDHS-206
  • 1,3-Benzenedicarboxamide, N1-(1-propyl-1H-benzimidazol-2-yl)-
  • Takinib >=98% (HPLC)
  • HepG2,malaria,MAP kinase kinase kinase, MEKK, MAPKKK,cancer,RASF,Inhibitor,arthritis,Takinib,inhibit,EDHS 206,HuH7,Apoptosis,EDHS206,RA-FLS,MAP3K
  • Takinib, 10 mM in DMSO
  • Takinib (EDHS-206) ，S8663
  • 1111556-37-6