Takinib
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).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.48%
- CAS 番号: 1111556-37-6
- 分子式: C18H18N4O2
- 分子量:322.36
-
保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
-
生物活性
-
化学情報
-
溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
-
Anti-Infection Compound Library
HY-L002
-
Apoptosis Compound Library
HY-L003
-
Immunology/Inflammation Compound Library
HY-L007
-
Kinase Inhibitor Library
HY-L009
-
MAPK Compound Library
HY-L010
-
Anti-Cancer Compound Library
HY-L025
-
Oxygen Sensing Compound Library
HY-L045
-
Pyroptosis Compound Library
HY-L059
-
Orally Active Compound Library
HY-L061
-
Anti-Breast Cancer Compound Library
HY-L074
-
Anti-Blood Cancer Compound Library
HY-L079
-
Anti-Obesity Compound Library
HY-L087
-
Targeted Diversity Library
HY-L099
-
Human Metabolite Library
HY-L123
-
Cancer Stem Cells Compound Library
HY-L135
-
Highly Selective Inhibitors Library
HY-L158
-
Highly Selective Activators Library
HY-L159
-
Cell Death Library
HY-L162
-
Serine/Threonine Kinase Inhibitor Library
HY-L164
-
Anti-Hematopathy Compound Library
HY-L171
-
Multi-Target Compound Library
HY-L176
-
Bioactive Compound Library Max
HY-L181
-
Kinase Inhibitor Library Mini
HY-L009M
-
MCE Bioactive Compound Library
HY-L001V
-
Bioactive Compound Library
HY-L001
-
Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
-
High-Throughput Bioactive Compound Library
HY-L205
-
Anti-Rheumatic Arthritis Compound Library
HY-L210
-
Mass Spectrometry Human Metabolite Library
HY-L215
-
Posttranslational Modification Library
HY-L226
MedChemExpress（MCE）の使用を引用している文献 Takinib
More- Nat Commun. 2024 Jun 27;15(1):5441. [Abstract]
- J Adv Res. 2024 Dec 9:S2090-1232(24)00565-4. [Abstract]
- ACS Cent Sci. 2018 Aug 22;4(8):982-995. [Abstract]
- Cell Death Dis. 2024 Jun 21;15(6):438. [Abstract]
- Int J Biol Macromol. 2026 Mar:349:150991. [Abstract]
- Acta Pharmacol Sin. 2026 Mar 11. [Abstract]
- EMBO J. 2021 Nov 2;40(21):e108028. [Abstract]
- Cell Death Discov. 2025 Jul 25;11(1):345. [Abstract]
- Cell Rep. 2024 Oct 8;43(10):114827. [Abstract]
- J Med Chem. 2025 Feb 13;68(3):2694-2719. [Abstract]
- Clin Transl Med. 2022 Jun;12(6):e850. [Abstract]
- Antioxidants (Basel). 2021 Nov 26;10(12):1898. [Abstract]
- Elife. 2022 Jun 28;11:e78044. [Abstract]
- J Cell Biol. 2018 Aug 6;217(8):2727-2742. [Abstract]
- Biochem Pharmacol. 2025 Jan 21:116764. [Abstract]
- J Ethnopharmacol. 2026 Jun 12:364:121516. [Abstract]
- J Am Heart Assoc. 2018 Dec 4;7(23):e03677. [Abstract]
- Drug Des Devel Ther. 2025 Sep 30:19:8843-8864. [Abstract]
- Int J Mol Sci. 2026 Apr 2;27(7):3232. [Abstract]
- Int Immunopharmacol. 2024 Dec 19:146:113842. [Abstract]
- Eur J Pharmacol. 2023 May 15:947:175679. [Abstract]
- Mol Oncol. 2023 Nov;17(11):2356-2379. [Abstract]
- J Biol Chem. 2020 Oct 16;295(42):14325-14342. [Abstract]
- Am J Pathol. 2024 Aug 31:S0002-9440(24)00328-6. [Abstract]
- NPJ Syst Biol Appl. 2023 Nov 16;9(1):57. [Abstract]
- Mol Biol Cell. 2018 Oct 1;29(20):2470-2480. [Abstract]
- Biol Pharm Bull. 2020 Nov 1;43(11):1643-1652. [Abstract]
- bioRxiv. 2026 May 26:2026.05.24.727500. [Abstract]
- bioRxiv. 2025 Oct 1.
- J Pers Med. 2021 Sep 11;11(9):906. [Abstract]
Customer Validation & Images
-
Bio/Physico-chemical Assay
-
Bio/Physico-chemical Assay
-
WB
-
RT-PCR
-
WB
MAP3K アイソフォーム固有の製品をすべて表示
More
生物活性
|
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) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| MPC-11 | GI50 |
8.5 μM
Compound: Takinib
|
Cytotoxicity against mouse MPC-11 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Blue assay
Cytotoxicity against mouse MPC-11 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Blue assay
|
[PMID: 38283221] |
| NCI-H929 | GI50 |
51 μM
Compound: Takinib
|
Cytotoxicity against human NCI-H929 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Blue assay
Cytotoxicity against human NCI-H929 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Blue assay
|
[PMID: 38283221] |
Takinib (10-10000 nM; 24 hours) induces apoptosis following TNF-α stimulation in MDA-MB-231 cells[1].
Takinib (10 μM; 0-1 hours) reduces phosphorylation of IKK and p65[1].
Takinib serves as a chemical starting point for the development of PfPK9 (KD(app) of 0.46 μM) inhibitors for malaria[3].
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[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:Breast cancer cell line MDA-MB-231
-
Concentration: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.
-
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; oral gavage; daily until 17 days) slows tumor growth in the Hodgkin lymphoma xenograft NSG mice[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
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.
化学情報
-
CAS 番号 1111556-37-6
-
性状 Solid
-
分子量 322.36
-
分子式 C18H18N4O2
-
Color White to off-white
-
SMILES
CCCN1C2=CC=CC=C2N=C1NC(C3=CC(C(N)=O)=CC=C3)=O
-
別名
EDHS-206
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (30)
-
Journal Impact Factor
-
Most Recent
-
Nat Commun
Podocyte OTUD5 alleviates diabetic kidney disease through deubiquitinating TAK1 and reducing podocyte inflammation and injury. [Abstract]2024 Jun 27;15(1):5441. PMID: 38937512
Takinib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Jun 27;15(1):5441. [Abstract]
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.
Takinib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Jun 27;15(1):5441. [Abstract]
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.
-
J Adv Res
Dual regulation of phaseol on osteoclast formation and osteoblast differentiation by targeting TAK1 kinase for osteoporosis treatment. [Abstract]2024 Dec 9:S2090-1232(24)00565-4. PMID: 39662728
Takinib purchased from MedChemExpress. Usage Cited in: J Adv Res. 2024 Dec 9:S2090-1232(24)00565-4. [Abstract]
The activity of ALP in MCOBs following a 14-day exposure to OM with or without Takinib.
Takinib purchased from MedChemExpress. Usage Cited in: J Adv Res. 2024 Dec 9:S2090-1232(24)00565-4. [Abstract]
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.
-
ACS Cent Sci
Immunomodulation of the NLRP3 Inflammasome through Structure-Based Activator Design and Functional Regulation via Lysosomal Rupture. [Abstract]2018 Aug 22;4(8):982-995. PMID: 30159395 -
Cell Death Dis
Regulator of G protein signaling 16 restrains apoptosis in colorectal cancer through disrupting TRAF6-TAB2-TAK1-JNK/p38 MAPK signaling. [Abstract]2024 Jun 21;15(6):438. PMID: 38906869
Takinib purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2024 Jun 21;15(6):438. [Abstract]
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.
-
Int J Biol Macromol
Rabies virus matrix protein hijacks the TGF-beta activated kinase 1 binding protein 2-p38 mitogen-activated protein kinase pathway to inhibit apoptosis and promote viral replication. [Abstract]2026 Mar:349:150991. PMID: 41713525 -
Acta Pharmacol Sin
2026 Mar 11. PMID: 41813972 -
EMBO J
2021 Nov 2;40(21):e108028. PMID: 34472622 -
Cell Death Discov
RIPK1 S213E mutant suppresses RIPK1-dependent cell death by preventing interactions with RIPK3 and CASP8. [Abstract]2025 Jul 25;11(1):345. PMID: 40715038 -
Cell Rep
Polo-like kinase 2 promotes microglial activation via regulation of the HSP90α/IKKβ pathway. [Abstract]2024 Oct 8;43(10):114827. PMID: 39383034 -
J Med Chem
Design and Synthesis of Hederagenin Derivatives for the Treatment of Sepsis by Targeting TAK1 and Regulating the TAK1-NF-κB/MAPK Signaling. [Abstract]2025 Feb 13;68(3):2694-2719. PMID: 39817810 -
Clin Transl Med
Uterus globulin associated protein 1 (UGRP1) binds podoplanin (PDPN) to promote a novel inflammation pathway during Streptococcus pneumoniae infection. [Abstract]2022 Jun;12(6):e850. PMID: 35652821 -
Antioxidants (Basel)
2021 Nov 26;10(12):1898. PMID: 34942999 -
Elife
Domain fusion TLR2-4 enhances the autophagy-dependent clearance of Staphylococcus aureus in the genetic engineering goat. [Abstract]2022 Jun 28;11:e78044. PMID: 35762728 -
J Cell Biol
Endosomal TLR3, TLR7, and TLR8 control neuronal morphology through different transcriptional programs. [Abstract]2018 Aug 6;217(8):2727-2742. PMID: 29777026 -
Biochem Pharmacol
Downregulation of RSAD2 ameliorates keratinocyte hyperproliferation and skin inflammation in psoriasis via the TAK1/NF-κB axis. [Abstract]2025 Jan 21:116764. PMID: 39848474 -
J Ethnopharmacol
Nephropathy 1 Formula (N1F) mitigates cisplatin-induced acute kidney injury by inhibiting TAK1-dependent NF-κB signaling. [Abstract]2026 Jun 12:364:121516. PMID: 41812937 -
J Am Heart Assoc
2018 Dec 4;7(23):e03677. PMID: 30571597 -
Drug Des Devel Ther
Emodin Alleviates Monocrotaline-Induced Pulmonary Arterial Hypertension by Directly Targeting TAK1. [Abstract]2025 Sep 30:19:8843-8864. PMID: 41049040 -
Int J Mol Sci
2026 Apr 2;27(7):3232. PMID: 41977413 -
Int Immunopharmacol
Astragaloside IV ameliorates atherosclerosis by targeting TAK1 to suppress endothelial cell proinflammatory activation. [Abstract]2024 Dec 19:146:113842. PMID: 39706043 -
Eur J Pharmacol
RIP2 inhibition alleviates lipopolysaccharide-induced septic cardiomyopathy via regulating TAK1 signaling. [Abstract]2023 May 15:947:175679. PMID: 36967078 -
Mol Oncol
Proximity proteomics reveals role of Abelson interactor 1 in the regulation of TAK1/RIPK1 signaling. [Abstract]2023 Nov;17(11):2356-2379. PMID: 36635880 -
J Biol Chem
2020 Oct 16;295(42):14325-14342. PMID: 32796029 -
Am J Pathol
Lipopolysaccharide Triggers Luminal Acidification to Promote Defense Against Bacterial Infection in Vaginal Epithelium. [Abstract]2024 Aug 31:S0002-9440(24)00328-6. PMID: 39222908 -
NPJ Syst Biol Appl
Modulating the dynamics of NFκB and PI3K enhances the ensemble-level TNFR1 signaling mediated apoptotic response. [Abstract]2023 Nov 16;9(1):57. PMID: 37973854 -
Mol Biol Cell
2018 Oct 1;29(20):2470-2480. PMID: 30091641
Takinib purchased from MedChemExpress. Usage Cited in: Mol Biol Cell. 2018 Oct 1;29(20):2470-2480. [Abstract]
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.
-
Biol Pharm Bull
Sinomenine Inhibited Interleukin-1β-Induced Matrix Metalloproteinases Levels via SOCS3 Up-Regulation in SW1353 Cells. [Abstract]2020 Nov 1;43(11):1643-1652. PMID: 32879146 -
bioRxiv
2026 May 26:2026.05.24.727500. PMID: 42244601 -
-
J Pers Med
GPR30 Activation by 17β-Estradiol Promotes p62 Phosphorylation and Increases Estrogen Receptor α Protein Expression by Inducing Its Release from a Complex Formed with KEAP1. [Abstract]2021 Sep 11;11(9):906. PMID: 34575683
溶剤 & 溶解度
DMSO : 2.5 mg/mL (7.76 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
純度とドキュメンテーション
-
データシート (292 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
-
取扱説明書 (2659 KB)
参考文献
[1]. Totzke J, et al. Takinib, a Selective TAK1 Inhibitor, Broadens the Therapeutic Efficacy of TNF-α Inhibition for Cancer and Autoimmune Disease. Cell Chem Biol. 2017 Aug 17;24(8):1029-1039. [Content Brief]
[2]. Scarneo SA, et.al. Pharmacological inhibition of TAK1, with the selective inhibitor takinib, alleviates clinical manifestation of arthritis in CIA mice. Arthritis Res Ther. 2019 Dec 17;21(1):292. [Content Brief]
[3]. Raphemot R, et al. Plasmodium PK9 Inhibitors Promote Growth of Liver-Stage Parasites. Cell Chem Biol. 2019 Mar 21;26(3):411-419.e7. [Content Brief]
[4]. Panipinto PM, et.al. Takinib Inhibits Inflammation in Human Rheumatoid Arthritis Synovial Fibroblasts by Targeting the Janus Kinase-Signal Transducer and Activator of Transcription 3 (JAK/STAT3) Pathway. Int J Mol Sci. 2021;22(22):12580. Published 2021 Nov 22. [Content Brief]
[5]. Song Z,et.al. Essential role of the linear ubiquitin chain assembly complex and TAK1 kinase in A20 mutant Hodgkin lymphoma. Proc Natl Acad Sci U S A. 2020 Nov 17;117(46):28980-28991. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.1021 mL | 15.5106 mL | 31.0212 mL | 77.5530 mL |
| 5 mM | 0.6204 mL | 3.1021 mL | 6.2042 mL | 15.5106 mL |
Powered by Bioz