Art. -Nr.: HY-10456

TAK-715

12 Cited Publications

Kundenbewertung

Based on 12 publication(s) in Google Scholar

TAK-715 is an orally active and potent p38 MAPK inhibitor with IC₅₀s of 7.1 nM, 200 nM for p38α and p38β, respectively. TAK-715 inhibits casein kinase I (CK1δ/ε) to regulate activation of Wnt/β-catenin signaling. TAK-715 shows good significant efficacy in a rat arthritis model.

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Reinheit: 99.76%
CAS. Nr.: 303162-79-0
Formel: C₂₄H₂₁N₃OS
Molecular Weight:399.51

Speicherung:

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

TAK-715 Chemical Structure

CAS. Nr.: 303162-79-0

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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
- Clinical Trial
Chemical Information
Publications (12)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]^[2]

p38α

7.1 nM (IC₅₀)

p38β

200 nM (IC₅₀)

p38δ

>10 μM (IC₅₀)

p38γ

>10 μM (IC₅₀)

CK1γ2

CK1ε

Alle p38 MAPK Isoform-spezifische Produkte anzeigen :

Alle Casein Kinase Isoform-spezifische Produkte anzeigen :

Alle Wnt Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
THP-1	IC₅₀	48 nM Compound: 8h	In vitro inhibitory activity against lipopolysaccharide-stimulated release of tumor necrosis factor alpha from human monocytic THP-1 cells In vitro inhibitory activity against lipopolysaccharide-stimulated release of tumor necrosis factor alpha from human monocytic THP-1 cells	[PMID: 16162000]

In Vitro

TAK-715 (compound 8h) inhibits LPS-stimulated release of TNF-α from THP-1 (IC₅₀=48 nM) and has no inhibitory activity for major CYPs, including CYP3A4. TAK-715 has no inhibition to p38γ/δ, JNK1, ERK1, IKKβ, MEKK1 or TAK1 (IC₅₀>10 μM of all)^[1].
TAK 715 (10 μM; 1 hour) inhibits Wnt-3a-induced hDvl2 phosphorylation and the hDvl2 shift in U2OS-EFC cells^[2].
TAK-715 (1 μM; pretreatment for 16 hours) dramatically suppresses Norepinephrine (NE)-stimulated induction of fibronectin, CTGF, and Snai1 expression in TGF-β1-treated HK-2 cells at both the mRNA and protein levels^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

TAK-715 (compound 8h; 3-30 mg/kg; PO) significantly reduces the secondary paw volume^[1].
TAK-715 (10 mg/kg; PO) has a C_max of 0.19 μg/mL and an AUC of 1.16 μg h/mL.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

7-week-old male Lewis rats with arthritis^[1]
Dosage:

3, 10, 30 mg/kg
Administration:

PO; single dose
Result:

Significantly reduced the secondary paw volume (25% inhibition)

Animal Model:

Rat^[1]
Dosage:

10 mg/kg (Pharmacokinetic Analysis)
Administration:

PO
Result:

Had a C_max of 0.19 μg/mL and an AUC of 1.16 μg•h/mL.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 303162-79-0
Appearance Solid
Molecular Weight 399.51
Formel C₂₄H₂₁N₃OS
Color White to off-white
SMILES

O=C(C1=CC=CC=C1)NC2=NC=CC(C3=C(N=C(S3)CC)C4=CC=CC(C)=C4)=C2
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Publications (12)

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Journal Impact Factor

Protein Cell

Anthrax lethal toxin and tumor necrosis factor-α synergize on intestinal epithelia to induce mouse death. [Abstract]

2024 Feb 1;15(2):135-148. PMID: 37855658
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
J Transl Med

Potential of CLSPN as a therapeutic target in melanoma: a key player in melanoma progression and tumor microenvironment. [Abstract]

2025 Apr 24;23(1):470. PMID: 40275302
J Invest Dermatol

TWEAK/Fn14 Signals Mediate Burn Wound Repair. [Abstract]

2019 Jan;139(1):224-234. PMID: 30081003
Drug Des Devel Ther

Andrographolide Inhibits Static Mechanical Pressure-Induced Intervertebral Disc Degeneration via the MAPK/Nrf2/HO-1 Pathway. [Abstract]

2023 Feb 20:17:535-550. PMID: 36845666
Front Pharmacol

Topical TWEAK Accelerates Healing of Experimental Burn Wounds in Mice. [Abstract]

2018 Jun 21:9:660. PMID: 29977207

TAK-715 purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2018 Jun 21:9:660. [Abstract]

By Western blotting, the α-SMA and palladin proteins are determined in cells that are pretreated with NF-κB (JSH-23), Wnt/β-catenin (XAV939), EGFR (erlotinib), p38 MAPK (TAK-715), and Smad3 (SIS3) inhibitors and are followed by TWEAK stimulation.
Sci Rep

Adult fibroblasts use aggresomes only in distinct cell-states. [Abstract]

2022 Sep 2;12(1):15001. PMID: 36056070
Poultry Sci

SC75741 antagonizes vesicular stomatitis virus, duck Tembusu virus, and duck plague virus infection in duck cells through promoting innate immune responses. [Abstract]

2021 May;100(5):101085. PMID: 33799115
FASEB J

Inhibition of α1-adrenoceptor reduces TGF-β1-induced epithelial-to-mesenchymal transition and attenuates UUO-induced renal fibrosis in mice. [Abstract]

2020 Nov;34(11):14892-14904. PMID: 32939891
Eur J Immunol

The immunosuppressive drug cyclosporin A has an immunostimulatory function in CD8+ T cells. [Abstract]

2024 Jul;54(7):e2350825. PMID: 38650034
Research Square Print

September 15th, 2022.
bioRxiv

July 24, 2021.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (125.15 mM; Need ultrasonic; 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

2.5031 mL

12.5153 mL

25.0307 mL

5 mM

0.5006 mL

2.5031 mL

5.0061 mL

10 mM

0.2503 mL

1.2515 mL

2.5031 mL

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.26 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 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]. Saito A, Yamamoto M. Acute oral toxicity of capsaicin in mice and rats[J]. The Journal of toxicological sciences, 1996, 21(3): 195-200.

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.5031 mL	12.5153 mL	25.0307 mL	62.5767 mL
	5 mM	0.5006 mL	2.5031 mL	5.0061 mL	12.5153 mL
	10 mM	0.2503 mL	1.2515 mL	2.5031 mL	6.2577 mL
	15 mM	0.1669 mL	0.8344 mL	1.6687 mL	4.1718 mL
	20 mM	0.1252 mL	0.6258 mL	1.2515 mL	3.1288 mL
	25 mM	0.1001 mL	0.5006 mL	1.0012 mL	2.5031 mL
	30 mM	0.0834 mL	0.4172 mL	0.8344 mL	2.0859 mL
	40 mM	0.0626 mL	0.3129 mL	0.6258 mL	1.5644 mL
	50 mM	0.0501 mL	0.2503 mL	0.5006 mL	1.2515 mL
	60 mM	0.0417 mL	0.2086 mL	0.4172 mL	1.0429 mL
	80 mM	0.0313 mL	0.1564 mL	0.3129 mL	0.7822 mL
	100 mM	0.0250 mL	0.1252 mL	0.2503 mL	0.6258 mL

TAK-715

12 Cited Publications

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TAK-715

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Publications Citing Use of MedChemExpress (MCE) TAK-715

Alle p38 MAPK Isoform-spezifische Produkte anzeigen

Alle Casein Kinase Isoform-spezifische Produkte anzeigen

Alle Wnt Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (12)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

TAK-715 Related Classifications

HY-10456 Related Classifications