1. MAPK/ERK Pathway
  2. p38 MAPK
  3. p38α-IN-12

p38α-IN-12 is an orally bioavailable p38α MAPK inhibitor, with an IC50 of 0.11 nM and a Ki of 0.2 nM against human targets. p38α-IN-12 inhibits the production of TNFα in cellular systems and exerts in vivo efficacy in acute mouse models.

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p38α-IN-12

p38α-IN-12 Chemical Structure

CAS No. : 630106-85-3

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Description

p38α-IN-12 is an orally bioavailable p38α MAPK inhibitor, with an IC50 of 0.11 nM and a Ki of 0.2 nM against human targets. p38α-IN-12 inhibits the production of TNFα in cellular systems and exerts in vivo efficacy in acute mouse models[1].

In Vitro

p38α-IN-12 (compound 2x) inhibits LPS-induced TNFα production in human peripheral blood mononuclear cells with an IC50 of 6 nM[1].
p38α-IN-12 does not significantly inhibit human CYP 450 isoforms 1A2, 2C9, 2C19, 2D6, or 3A4, with IC50 values >40 μM for each[1].
p38α-IN-12 shows excellent metabolic stability in human and rat liver microsomes[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Parmacokinetics
Species Dose Route Bioavailability Clearance (CL) Vd T1/2
Mice[1] 10 mg/kg p.o. 60 % 0.3 1.3 L/kg 4.1 h
Molecular Weight

411.43

Formula

C22H17N7O2

CAS No.
SMILES

O=C(NC1=NOC=C1)C2=CC=C(C(=C2)NC3=NC=NC4=C3C=NN4C=5C=CC=CC5)C

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Room temperature in continental US; may vary elsewhere.

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

Purity & Documentation
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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p38α-IN-12
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HY-183042
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