Successful, we will reply to you quickly.OK
Please select the quantity.OK
Your message is being sent, please wait.Close
Send mail failed, please send again!Close
Products are for research use only. Not for human use. We do not sell to patients.
(TAK 715; TAK715)
TAK-715 Chemical Structure
|Product name: TAK-715|
|Cat. No.: HY-10456|
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.
IC50 value: 7.1 nM 
Target: p38α MAPK
in vitro: TAK 715 inhibits LPS-stimulated release of TNF-alpha from THP-1 with IC50 of 48 nM . TAK 715 (10 μM) inhibits Wnt-3a-induced hDvl2 phosphorylation and the hDvl2 shift in U2OS-EFC cells . 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 .
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 .
|M.Wt||399.51||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
DMSO: >15 mg/mL
|1 mg||5 mg||10 mg|
|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|
. Miwatashi S, et al. Novel inhibitor of p38 MAP kinase as an anti-TNF-alpha drug: discovery of N-[4-[2-ethyl-4-(3-methylphenyl)-1,3-thiazol-5-yl]-2-pyridyl]benzamide (TAK-715) as a potent and orally active anti-rheumatoid arthritis agent. J Med Chem, 2005, 48(19), 5966-5979.
Doramapimod (BIRB 796) is a highly selective p38(alpha) MAPK inhibitor with Kd of 0.1 nM, 330-fold greater selectivity versus JNK2, weak inhibition for c-RAF, Fyn and Lck, insignificant inhibition of ERK-1, SYK, IKK2, ZAP-70, EGFR, HER2, PKA, PKC, PKC(alpha)/(beta)/(gamma).
Losmapimod (GW856553X; SB856553; GSK-AHAB) is a selective, potent, and orally active p38 MAPK inhibitor with pKi of 8.1 and 7.6 for p38(alpha) and p38(beta), respectively.
p38 MAPK-IN-1 is a novel potent and selective inhibitor of p38 MAPK with IC50 of 68 nM, shows sustained levels, low clearance and good bioavailability.
Pamapimod is a novel p38 mitogen-activated protein kinase inhibitor.
PD 169316 is a potent, cell-permeable and selective p38 MAP kinase inhibitor (IC50 = 89 nM).
SB 202190 is a highly selective, potent and cell-permeable inhibitor of p38 MAP kinase with IC50 values of 50 nM and 100 nM for p38(alpha) and p38(beta) respectively; also showed slightly weaker activity for BRD4 (Kd=3.4 uM).
SB 239063 is a potent and selective p38 MAPK inhibitor (IC50 = 44 nM for p38(alpha)). SB 239063 displays > 220-fold selectivity over ERK, JNK1 and other kinases; ~ 3-fold more selective than SB 203580.
SB-242235 is a potent and selective p38 MAP kinase inhibitor with IC50 of 1.0 uM.
SCIO-469 is a selective ATP-competitive p38 inhibitor with IC50 of 9 nM for p38(alpha)in vitro, about 10-fold selectivity for p38(alpha) over p38(beta), and at least 2000-fold selectivity for p38(alpha) over an in vitro panel of 20 other kinases, including other MAK kinases.