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Cat. No.: HY-183042

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p38α-IN-12

p38α-IN-12 is an orally bioavailable p38α MAPK inhibitor, with an IC₅₀ of 0.11 nM and a K_i 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.

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

CAS No.: 630106-85-3
Formula: C₂₂H₁₇N₇O₂
Molecular Weight:411.43

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

p38α-IN-12 Chemical Structure

CAS No.: 630106-85-3

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- Cellular Effect
- In Vitro
- Parmacokinetics
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
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Biological Activity

Description

All p38 MAPK Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
PBMC	IC₅₀	6 nM Compound: 2x	Inhibition of LPS-induced TNFalpha production in human PBMC Inhibition of LPS-induced TNFalpha production in human PBMC	[PMID: 18359226]

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)	V_d	T_1/2
Mice^[1]	10 mg/kg	p.o.	60 %	0.3	1.3 L/kg	4.1 h

Chemical Information

CAS No. 630106-85-3
Molecular Weight 411.43
Formula C₂₂H₁₇N₇O₂
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.
Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Das J, et al. Pyrazolo-pyrimidines: A novel heterocyclic scaffold for potent and selective p38α inhibitors[J]. Bioorganic & medicinal chemistry letters, 2008, 18(8): 2652-2657.

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How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
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p38α-IN-12

All p38 MAPK Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

p38α-IN-12 Related Classifications

HY-183042 Related Classifications