GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

PS540446 | Pyrrolo[2,​1-​f]​[1,​2,​4]​triazine-​6-​carboxamide, 4-​[[5-​[(cyclopropylamino)​carbonyl]​-​2-​methylphenyl]​amino]​-​5-​methyl-​N-​propyl-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

BMS-582949 BMS-582949 (PS540446) is a potent and selective p38 mitogen-activated protein kinase (p38 MAPK) inhibitor with IC50 of 13nM,inhibiting both p38 kinase activity and activation of p38.
In vitro

BMS-582949 is found to inhibit p38 activation in cells, as measured by phosphorylation of p38. BMS-582949 treatment of cells in which p38 has been activated by LPS rapidly reversed p38 activation as shown by loss of phosphorylation of p38. BMS-582949 is therefore a dual action p38 kinase inhibitor, inhibiting both p38 kinase activity and p38 activation in cells. BMS-582949 binding to p38a results in a conformational change of the activation loop which is phosphorylated by upstream kinases, therefore it inhibits phosphorylation of p38 by upstream MKK by inducing a less accessible conformation of the activation loop.

In vivo

The mouse clearance rate for BMS-582949 is 4.4 mL/min/kg. And at an oral dose of 10 mg/kg, the mouse AUC0-8 h for BMS-582949 is 75.5 μM•h. BMS-582949 exhibited oral bioavailability values of 90% and 60% in mice and rats, respectively.
Cell Data

cell lines：Human colon carcinoma cell line HT-29

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Synonyms

PS540446 | Pyrrolo[2, ​1-​f]​[1, ​2, ​4]​triazine-​6-​carboxamide, 4-​[[5-​[(cyclopropylamino)​carbonyl]​-​2-​methylphenyl]​amino]​-​5-​methyl-​N-​propyl-

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

BMS-582949 (PS540446) is a potent and selective p38 mitogen-activated protein kinase (p38 MAPK) inhibitor with IC50 of 13nM, inhibiting both p38 kinase activity and activation of p38.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

INHIBITOR

Mechanism of action

MAP kinase p38 alpha inhibitor

Product Properties

• ALogP: 3.269
• hba_count: 4
• HBD Count: 3
• Rotatable Bond: 7

Names and Identifiers

• Isomeric SMILES: CCCNC(=O)C1=CN2C(=C1C)C(=NC=N2)NC3=C(C=CC(=C3)C(=O)NC4CC4)C
• Molecular Weight: 406.48
• Reaxy-Rn: 11821218
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=11821218&ln=

Associated Targets(Human)

MAPK14 Tchem Mitogen-activated protein kinase 14 (3 Activities)

Discover Target: MAPK14

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemical and Physical Properties

• DMSO(mg / mL) Max Solubility: 81
• DMSO(mM) Max Solubility: 199.2717969
• Water(mg / mL) Max Solubility: ＜1