Art. -Nr.: HY-103490

Takinib

(Synonyms: EDHS-206)

30 Cited Publications

Kundenbewertung

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 (K_D(app) of 0.46 μM).

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Reinheit: 99.48%
CAS. Nr.: 1111556-37-6
Formel: C₁₈H₁₈N₄O₂
Molecular Weight:322.36

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Takinib Chemical Structure

CAS. Nr.: 1111556-37-6

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (30)
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

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)

Alle MAP3K Isoform-spezifische Produkte anzeigen :

Cellular Effect

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]

In Vitro

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 (K_D(app) of 0.46 μM) inhibitors for malaria^[3].
Takinib (2 hours; 0.1-20 μM; human RASFs) induces phosphorylation of TAK1^Thr184/187, STAT3^Tyr705 and STAT3^Ser727 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.

Western Blot Analysis^[1]

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.

Western Blot Analysis^[4]

Cell Line:

IL-1β-treated (10 ng/mL; 30 min) RASFs
Concentration:

0.1-20 µM
Incubation Time:

2 hours
Result:

Induced phosphorylation of TAK1^Thr184/187, STAT3^Tyr705 and STAT3^Ser727.

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].

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.

Chemical Information

CAS. Nr. 1111556-37-6
Appearance Solid
Molecular Weight 322.36
Formel C₁₈H₁₈N₄O₂
Color White to off-white
SMILES

CCCN1C2=CC=CC=C2N=C1NC(C3=CC(C(N)=O)=CC=C3)=O
Synonyms

EDHS-206
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (30)

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Journal Impact Factor

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

Sonic Hedgehog-Gli1 signaling promotes microglial activation via the IKKβ/NF-κB pathway. [Abstract]

2026 Mar 11. PMID: 41813972
EMBO J

CARS senses cysteine deprivation to activate AMPK for cell survival. [Abstract]

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)

Glucose Activates Lysine-Specific Demethylase 1 through the KEAP1/p62 Pathway. [Abstract]

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

CD40L Priming of Platelets via NF-κB Activation is CD40- and TAK1-Dependent. [Abstract]

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

MK2/p38/p53 Suppress Basal IL-1β and Non-Canonical NF-κB Signaling in Macrophages. [Abstract]

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

An alternative model for type I interferon induction downstream of human TLR2. [Abstract]

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

WDR62 mediates TNFα-dependent JNK activation via TRAF2-MLK3 axis. [Abstract]

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

Squamous-state excursions activate APOBEC3A in cancer. [Abstract]

2026 May 26:2026.05.24.727500. PMID: 42244601
bioRxiv

2025 Oct 1.
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

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.1021 mL

15.5106 mL

31.0212 mL

5 mM

0.6204 mL

3.1021 mL

6.2042 mL

10 mM

---

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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
DMSO	5 mM	0.6204 mL	3.1021 mL	6.2042 mL	15.5106 mL

Keywords

Takinib

30 Cited Publications

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Takinib

Anti-Infection Compound Library

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

Anti-Cancer Compound Library

Oxygen Sensing Compound Library

Pyroptosis Compound Library

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Obesity Compound Library

Targeted Diversity Library

Human Metabolite Library

Cancer Stem Cells Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Kinase Inhibitor Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Mass Spectrometry Human Metabolite Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) Takinib

Alle MAP3K Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (30)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Takinib Related Classifications

Art. -Nr.: HY-103490