1. MAPK/ERK Pathway
  2. p38 MAPK
  3. RWJ-67657

RWJ-67657 (Synonyms: JNJ 3026582)

Cat. No.: HY-15505
Handling Instructions

RWJ-67657 (JNJ 3026582) is an orally active and selective p38α and p38β MAPK inhibitor with IC50s of 1 and 11 μM, respectively. RWJ-67657 displays no activity at p38γ and p38δ, and exhibits cardio protective effect. Anti-inflammatory and anti-tumor activity.

For research use only. We do not sell to patients.

RWJ-67657 Chemical Structure

RWJ-67657 Chemical Structure

CAS No. : 215303-72-3

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10 mM * 1 mL in DMSO USD 453 In-stock
Estimated Time of Arrival: December 31
5 mg USD 500 In-stock
Estimated Time of Arrival: December 31
10 mg USD 850 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

RWJ-67657 (JNJ 3026582) is an orally active and selective p38α and p38β MAPK inhibitor with IC50s of 1 and 11 μM, respectively. RWJ-67657 displays no activity at p38γ and p38δ, and exhibits cardio protective effect. Anti-inflammatory and anti-tumor activity[1].

IC50 & Target[1]

p38α

1 μM (IC50)

p38β

11 μM (IC50)

In Vitro

RWJ-67657 inhibits the release of TNF-α by lipopolysaccharide (LPS)-treated human peripheral blood mononuclear cells with an IC50 of 3 nM, as well as the release of TNF-α from peripheral blood mononuclear cells treated with the superantigen staphylococcal enterotoxin B, with an IC50 value of 13 nM[2].
RWJ67657 (10 μM; 24 hours) decreases colony formation in MCF-7 cells[3].

Cell Proliferation Assay[3]

Cell Line: MCF-7 breast carcinoma cells
Concentration: 10 μM
Incubation Time: 24 hours
Result: Decreased colony formation.
In Vivo

RWJ-67657 inhibits 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[2].
RWJ-67657 (50 mg/kg; administered orally; once per day for 7 consecutive days) displays a potent anti-inflammatory effect. By both improving the functioning of endothelial progenitor cells (EPCs) and reducing inflammation, EPC transplantation plus RWJ-67657 administration synergistically promotes angiogenesis and neurogenesis after diabetic stroke[4].

Animal Model: The db/db mice (male, 8 weeks old) with EPCs[4]
Dosage: 50 mg/kg
Administration: Administered orally; once per day for 7 consecutive days
Result: Increased angiogenesis and neurogenesis of diabetic mice after cotreatment with EPCs transplantation.
Molecular Weight

425.50

Formula

C₂₇H₂₄FN₃O

CAS No.

215303-72-3

SMILES

OCCC#CC1=NC(C2=CC=C(F)C=C2)=C(C3=CC=NC=C3)N1CCCC4=CC=CC=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

RWJ-67657JNJ 3026582RWJ67657RWJ 67657JNJ3026582JNJ-3026582p38 MAPKp38αp38βcardioprotective. Anti-inflammatoryanti-tumorinflammationMCF-7Inhibitorinhibitorinhibit

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RWJ-67657
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HY-15505
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