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VX 745

Catalog #: 3915
5 Citations Datasheet
Catalog # Availability Size / Price Qty
3915/10
3915/50
VX 745 | CAS No. 209410-46-8 | p38 Inhibitors
1 Image
Description: Potent and selective p38α inhibitor
Alternative Names: VX745,VX-745,Neflamapimod

Chemical Name: 5-(2,6-Dichlorophenyl)-2-[2,4-difluorophenyl)thio]-6H-pyrimido[1,6-b]pyridazin-6-one

Purity: ≥98%

Product Details
Citations (5)
Reviews
Biological Activity Technical Data Background Product Datasheets Calculators

Biological Activity

VX 745 is a highly potent and selective p38α/MAPK14 inhibitor, also inhibits p38β (IC50 values are 10 nM and 220 nM respectively). VX 745 blocks TNFα production in LPS-stimulated HWB in vitro (IC50 = 51-180 nM). Also reduces phosphorylation of p38MAPKα and the downstream target Hsp27, leading to vasodilation, reduces IL-1β levels and amyloid plaques in cortex and hippocampus and lowers CSF tau levels in vivo.

External Portal Information

Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of VX 745 is reviewed on the chemical probes website.

Technical Data

M.Wt:
436.26
Formula:
C19H9Cl2F2N3OS
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
209410-46-8

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. The inflammatory kinase MAP4K4 promotes reactivation of Kaposi's sarcoma herpesvirus and enhances the invasiveness of infected endothelial cells.
    Haas D, Bala K, Busche G, Weidner-Glunde M, Santag S, Kati S, Gramolelli S, Damas M, Dittrich-Breiholz O, Kracht M, Ruckert J, Varga Z, Keri G, Schulz T
    PLoS Pathog, 2013;9(11):e1003737.
  2. Rapid synthesis of VX-745: p38 MAP kinase inhibition in Werner syndrome cells.
    Bagley et al.
    Bioorg.Med.Chem.Lett., 2007;17:5107
  3. Selective p38alpha inhibitors clinically evaluated for the treatment of chronic inflammatory disorders.
    Goldstein et al.
    J.Med.Chem., 2010;53:2345

Product Datasheets

Citations for VX 745

The citations listed below are publications that use Tocris products. Selected citations for VX 745 include:

5 Citations: Showing 1 - 5

  1. CDK4/6 inhibitor-mediated cell overgrowth triggers osmotic and replication stress to promote senescence.
    Authors: Crozier Et al.
    Mol.Cell  2023;83:4062
  2. Increased ACTL6A occupancy within mSWI/SNF chromatin remodelers drives human squamous cell carcinoma.
    Authors: Gerald R Et al.
    Mol Cell  2021;81:4964-4978.e8
  3. CDK8 Fine-Tunes IL-6 Transcriptional Activities by Limiting STAT3 Resident Time at the Gene Loci.
    Authors: Ignacio Et al.
    Cell Rep  2020;33:108545
  4. Differential effect of p38 and MK2 kinase inhibitors on the inflammatory and toxicity biomarkers in vitro.
    Authors: Singh Et al.
    Hum Exp Toxicol  2018;37:521
  5. The inflammatory kinase MAP4K4 promotes reactivation of Kaposi's sarcoma herpesvirus and enhances the invasiveness of infected endothelial cells.
    Authors: Haas Et al.
    PLoS Pathog  2013;9:e1003737

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