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MW 436.3 Da. Potent, selective p38 alpha MAPK inhibitor (IC50 = 10 nM), with 20-fold selectivity over p38 beta and 1000-fold selectivity over closely related kinases, ERK1 and JNK1-3.

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Images

Chemical Structure - VX-745, p38 alpha MAPK inhibitor (AB230367), expandable thumbnail

Key facts

CAS number
209410-46-8
Form
Solid
Molecular weight
436.3 Da
Molecular formula
C19H9Cl2F2N3OS
PubChem identifier
3038525
Nature
Synthetic

Target data

Alternative names

ADRA2RL1, ADRARL1, Alpha 2 adrenergic receptor subtype C2, Alpha 2B adrenoceptor, Alpha 2B adrenoreceptor, Alpha-PAK, Beta PAK, CAM kinase II delta, CAMK 2, CAMK 2B, CAMK 2d, CAMK2G, CAMKA, CDKN1A, CSAID Binding Protein 1, CSAID-binding protein, CSBP, CSBP 1, CSBP 2, CSPB1, CaM kinase II, CaM kinase II alpha, CaM kinase II beta, CaM kinase II gamma, CaM kinase II subunit alpha, CaMK-II subunit alpha, Calcium / calmodulin dependent protein kinase II delta, Calcium/calmodulin dependent protein kinase II gamma, Calcium/calmodulin-dependent protein kinase II-alpha, Calcium/calmodulin-dependent protein kinase type II subunit alpha, Camk2a, Csaids binding protein, Cytokine suppressive anti-inflammatory drug-binding protein, EC 2.7.11.1, EXIP, GSD9C, Gamma-PAK, Germinal center kinase like kinase, Germinal center kinase-related protein kinase, KCC2A_HUMAN, KHS, Kinase homologous to SPS1/STE20, MAP kinase 14, MAP kinase MXI2, MAP kinase p38 alpha, MAP4K3, MAPK 14, MAPK/ERK kinase kinase kinase 3, MAPK/ERK kinase kinase kinase 5, MAPKKKK3, MAX-interacting protein 2, MEK kinase kinase 3, MEK kinase kinase 5, MEKKK 3, MEKKK 5, MK14_HUMAN, MRX30, MRX47, Mitogen-activated protein kinase 14, Mitogen-activated protein kinase p38 alpha, Mxi 2, OPHN3, Oligophrenin 3, P21 (CDKN1A) activated kinase 2, P21 (CDKN1A) activated kinase 3, P21 protein (Cdc42/Rac) activated kinase 1, P21 protein (Cdc42/Rac) activated kinase 3, P21/Cdc42/Rac1 activated kinase 1 (yeast Ste20 related), P38, P58, PAK alpha, PAK3beta, PAK65, PAKgamma, PHK gamma LT, PHK gamma T, PRKM14, PRKM15, PSK C3, Phosphorylase b kinase gamma catalytic chain testis/liver isoform, Phosphorylase b kinase gamma catalytic chain, liver/testis isoform, Phosphorylase kinase catalytic subunit gamma 2, Phosphorylase kinase gamma subunit 2, Phosphorylase kinase subunit gamma 2, Phosphorylase kinase, gamma 2 (testis), Phosphorylase kinase, gamma 2 (testis/liver), RAB8IPL1, RK, S6/H4 kinase, SAPK2A, STE20 homolog, yeast, Serine/threonine protein kinase PAK 2, Serine/threonine protein kinase PAK 3, Serine/threonine protein kinase PHKG2, Serine/threonine-protein kinase PAK 1, Stress-activated protein kinase 2a, alpha 2BAR, bPAK, calcium/calmodulin-dependent protein kinase II beta, hPAK3, mitogen-activated protein kinase kinase kinase kinase 3, p21 activated kinase 3, p21 protein (Cdc42/Rac)-activated kinase 2, p21-activated kinase 1, p21-activated kinase 2, p21/Cdc42/Rac1-activated kinase 1 (STE20 homolog, yeast), p38 ALPHA, p38 MAP kinase, p38 MAPK, p38 mitogen activated protein kinase, p38alpha Exip, p65-PAK

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MW 436.3 Da. Potent, selective p38 alpha MAPK inhibitor (IC50 = 10 nM), with 20-fold selectivity over p38 beta and 1000-fold selectivity over closely related kinases, ERK1 and JNK1-3.

Key facts

PubChem identifier
3038525
Solubility

VX-745 has a solubility of approximately 0.5 mg/ml in a 1:1 solution of DMF:PBS (pH 7.2). We do not recommend storing the aqueous solution for more than one day.

Biochemical name
Neflamapimod
Biological description

Potent, selective p38 alpha MAPK inhibitor (IC50 = 10 nM), with 20-fold selectivity over p38 beta and 1000-fold selectivity over closely related kinases, ERK1 and JNK1-3.

Canonical SMILES
C1=CC(=C(C(=C1)Cl)C2=C3C=CC(=NN3C=NC2=O)SC4=C(C=C(C=C4)F)F)Cl
InChI
InChI=1S/C19H9Cl2F2N3OS/c20-11-2-1-3-12(21)17(11)18-14-5-7-16(25-26(14)9-24-19(18)27)28-15-6-4-10(22)8-13(15)23/h1-9H
InChIKey
VEPKQEUBKLEPRA-UHFFFAOYSA-N
IUPAC name
5-(2,6-dichlorophenyl)-2-(2,4-difluorophenyl)sulfanylpyrimido[1,6-b]pyridazin-6-one

Storage

Shipped at conditions
Blue Ice
Appropriate short-term storage conditions
-20°C
Appropriate long-term storage conditions
-20°C

Supplementary info

This supplementary information is collated from multiple sources and compiled automatically.
Activity summary

P38 also known as MAPK14 is a mitogen-activated protein kinase with a mass of approximately 41 kDa. It is part of the larger family of MAP kinases which play an essential role in cellular responses to external stress signals. You can find p38 widely expressed in different tissues including heart brain and skeletal muscle. It exhibits its functions by becoming activated through phosphorylation and participating in signaling cascades that control various cellular functions.

Biological function summary

P38 kinase and other components like ADRA2B PAK1-3 CaMKII PHKG2 MAP4K5 and MAP4K3/GLK contribute to cell survival apoptosis and inflammatory responses. They can be part of multi-protein complexes integrating signals that control cellular activities such as motility proliferation and differentiation. For instance CaMKII a calcium/calmodulin-dependent kinase has a mass around 55 to 60 kDa and influences neuronal signaling while ADRA2B an adrenergic alpha-2B receptor modulates vasoconstriction and neurotransmitter release.

Pathways

Many of these targets participate in the MAPK signaling and calcium signaling pathways. p38 interacts closely with upstream kinases like MAP4K3/GLK to propagate stress signals while PAK1 relates with Rac and Cdc42 GTPases playing a role in cytoskeletal reorganization. CaMKII acts in calcium signaling linking calcium influx to downstream events and often working alongside proteins such as calmodulin. These interactions coordinate complex cellular responses that depend on immediate and precise control of signaling pathways.

Associated diseases and disorders

P38 and related proteins are linked to inflammatory diseases and neurodegenerative disorders. For example aberrant p38 activity associates with rheumatoid arthritis due to its role in promoting inflammatory cytokine production. Parkinson's disease shows correlation with PAK kinases particularly PAK1 which affects neural plasticity. Dysregulation within these pathways often involves additional proteins like CaMKII whose misregulation can exacerbate disease progression affecting the overall outcome for the individual.

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1 product image

  • Chemical Structure - VX-745, p38 alpha MAPK inhibitor (ab230367), expandable thumbnail

    Chemical Structure - VX-745, p38 alpha MAPK inhibitor (ab230367)

    2D chemical structure image of ab230367, VX-745, p38 alpha MAPK inhibitor

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Product protocols

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