RWJ 67657|p38 MAPK inhibitor|DC Chemicals

Cas No.:	215303-72-3
Chemical Name:	4-[4-(4-Fluorophenyl)-1-(3-phenylpropyl)-5-(4-pyridinyl)-1H-imidazol-2-yl]-3-butyn-1-ol
Synonyms:	RWJ-67657; RWJ-67657; RWJ-67657
SMILES:	C(O)CC#CC1N(CCCC2=CC=CC=C2)C(C2C=CN=CC=2)=C(C2=CC=C(F)C=C2)N=1
Formula:	C₂₇H₂₄FN₃O
M.Wt:	425.5
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

RWJ-67657 is a potent p38 MAPK inhibitor, which inhibited the release of TNF-alpha by lipopolysaccharide (a monocyte stimulus)-treated human peripheral blood mononuclear cells with an IC(50) of 3 nM, as well as the release of TNF-alpha from peripheral blood mononuclear cells treated with the superantigen staphylococcal enterotoxin B (a T cell stimulus), with an IC(50) value of 13 nM. This compound was approximately 10-fold more potent than the literature standard p38 kinase inhibitor SB 203580 in all p38 dependent in vitro systems tested. RWJ 67657 inhibited the enzymatic activity of recombinant p38alpha and beta, but not gamma or delta, in vitro and had no significant activity against a variety of other enzymes. In contrast, SB 203580 significantly inhibited the tyrosine kinases p56 lck and c-src (IC(50) = 5 microM). RWJ 67657 did not inhibit T cell production of interleukin-2 or interferon-gamma and did not inhibit T cell proliferation in response to mitogens. RWJ 67657 inhibited TNF-alpha production in lipopolysaccharide-injected mice (87% inhibition at 50 mg/kg) and in rats (91% inhibition at 25 mg/kg) after oral administration. Based on these favorable biological properties, RWJ 67657 may have use as a treatment For inflammatory diseases. (copied from J Pharmacol Exp Ther. 1999 Nov;291(2):680-7.) (12/2/2013).For the detailed information of RWJ67657, the solubility of RWJ67657 in water, the solubility of RWJ67657 in DMSO, the solubility of RWJ67657 in PBS buffer, the animal experiment (test) of RWJ67657, the cell expriment (test) of RWJ67657, the in vivo, in vitro and clinical trial test of RWJ67657, the EC50, IC50,and Affinity of RWJ67657, Please contact DC Chemicals.

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2018-0101

Cat. No.	Product name	Field of application
DC74347	NC-p38i NC-37	Non-canonical p38α inhibitor NC-37 (NC-p38i NC-37) is a potent, highly selective, non-canonical inhibitor of p38α, inhibits TAB1-induced p38α autophosphorylation in vitro with IC50 of 0.27 uM.
DC48953	Emprumapimod	Emprumapimod is a potent, orally bioavailable and selective inhibitor of p38α MAPK directly inhibits LPS-induced IL-6 production from RPMI-8226 cell (IC50=100 pM). Emprumapimod can be used for the research of dilated cardiomyopathy and acute inflammatory pain.
DC7028	SB242235	SB-242235 is a potent and selective p38 MAP kinase inhibitor with IC50 of 1.0 uM.
DC4173	VX-745	VX-745 is a potent and selective inhibitor of p38α MAPK and p38β MAPK with IC50 of 10 nM and 220 nM, respectively.
DC1061	VX-702 (VX702)	VX-702 is a highly selective inhibitor of p38 MAPKα with IC50 of 4-20 nM.
DC9300	TA-02	TA-02 induces cardiomyocyte differentiation from human embryonic stem cells following mesoderm induction. Potently inhibits p38α, CK1δ and CK1ε (IC50 values are 20, 32 and 32 nM respectively).
DC7946	SKF-86002	SKF-86002 is a potent inhibitor of p38 MAP kinase wit IC50 of 0.5-1 uM; inhibits LPS-induced IL-1 and TNF-α production in human monocytes (IC50 = 1 μM).
DC8255	SD-06	SD-06 is a p38 MAP kinase inhibitor; inhibits p38α with an IC50 value of 170 nM and inhibits LPS-stimulated TNF-release in rats (83% inhibition at 1mg/kg, po).
DC1004	SB-203580	SB203580 is a p38 MAPK inhibitor with IC50 of 0.3-0.5 μM and blocks PKB phosphorylation with IC50 of 3-5 μM.
DC7807	SB 239063	SB 239063 is a potent and selective p38 MAPK inhibitor (IC50 = 44 nM for p38α). SB 239063 displays > 220-fold selectivity over ERK, JNK1 and other kinases; ~ 3-fold more selective than SB 203580.