TAK-715

Name: TAK-715
Brand: Selleck Chemicals
SKU: S2928
Rating: 5 (1 reviews)

For research use only. Not for use in humans.

Catalog No.S2928

1 publication

Molecular Weight(MW): 399.51

TAK-715 is a p38 MAPK inhibitor for p38α with IC50 of 7.1 nM, 28-fold more selective for p38α over p38β, no inhibition to p38γ/δ, JNK1, ERK1, IKKβ, MEKK1 or TAK1. Phase 2.

Selleck's TAK-715 has been cited by 1 publication

Nat Cell Biol, 2019, 21(6):778-790

PubMed: 31160710

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Biological Activity

Description

TAK-715 is a p38 MAPK inhibitor for p38α with IC50 of 7.1 nM, 28-fold more selective for p38α over p38β, no inhibition to p38γ/δ, JNK1, ERK1, IKKβ, MEKK1 or TAK1. Phase 2.

Targets

p38α ^[1] (Cell-free assay)	p38β ^[1] (Cell-free assay)
7.1 nM	0.20 μM

In vitro

TAK 715 inhibits LPS-stimulated release of TNF-alpha from THP-1 with IC50 of 48 nM. ^[1] TAK 715 (10 μM) inhibits Wnt-3a-induced hDvl2 phosphorylation and the hDvl2 shift in U2OS-EFC cells. ^[2] The amide NH of TAK 715 is hydrogen bonded to the main-chain carbonyl of Met109 of p38 alpha. TAK 715 binds relatively high in the ATP pocket, occupying the hydrophobic back pocket, the adenine region and the front pocket of p38 as well as extending to most of the length of the Gly-rich loop. ^[3]

In vivo

TAK 715 (10 mg/kg, po) inhibits LPS-induced TNF-alpha production in mice with 87.6% inhibition. TAK 715 has a modest mouse bioavailability of 18.4% and a slightly improved rat bioavailability of 21.1%. TAK 715 has a modest mouse bioavailability of 18.4% and a slightly improved rat bioavailability of 21.1%. TAK 715 results in Cmax of 0.19 μg/mL and AUC(0-24 hours) of 1.16 μg·h/mL in rats. TAK 715 (30 mg/kg, po) significantly reduces the secondary paw volume with 25 % inhibition in a rat adjuvant-induced arthritis (AA) model. ^[1]

Protocol

Animal Research:^[1]	- Collapse Animal Models: Adjuvant-induced arthritis (AA) rat model Formulation: Saline Dosages: 30 mg/kg Administration: Orally (Only for Reference)

References

Solubility (25°C)

In vitro	DMSO	80 mg/mL (200.24 mM)
	Ethanol	16 mg/mL (40.04 mM)
	Water	Insoluble
In vivo	Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 30% propylene glycol, 5% Tween 80, 65% D5W For best results, use promptly after mixing.	30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information Download TAK-715 SDF

Molecular Weight	399.51
Formula	C₂₄H₂₁N₃OS
CAS No.	303162-79-0
Storage	3 years -20°C powder
Storage	2 years -80°C in solvent
Synonyms	N/A
Smiles	CCC1=NC(=C(S1)C2=CC(=NC=C2)NC(=O)C3=CC=CC=C3)C4=CC=CC(=C4)C

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p38 MAPK Signaling Pathway Map

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TAK-715