An inhibitor of PAK1 activation
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IPA-3

Item No. 14759

Technical Information
Formal Name
1,1'-dithiobis-2-naphthalenol
CAS Number
42521-82-4
Synonyms
  • Inhibitor of PAK1 Activation 3
Molecular Formula
C20H14O2S2
Formula Weight
Purity
≥95%
A crystalline solid
DMF: 5 mg/mlDMF:PBS (pH 7.2) (1:4): 0.2 mg/mlDMSO: 5 mg/ml
λmax
223, 357 nm
SMILES
OC1=C(SSC2=C(O)C=CC3=C2C=CC=C3)C4=CC=CC=C4C=C1
InChi Code
InChI=1S/C20H14O2S2/c21-17-11-9-13-5-1-3-7-15(13)19(17)23-24-20-16-8-4-2-6-14(16)10-12-18(20)22/h1-12,21-22H
InChi Key
RFAXLXKIAKIUDT-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    IPA-3 is an allosteric inhibitor of p21-activated kinase 1 (PAK1) activation (IC50 = 2.5 µM) that does not inhibit pre-activated PAK1.1 It selectively inhibits activation of the group I PAKs, PAK1, PAK2, and PAK3 over the group II PAKs, PAK4, PAK5, and PAK6 at 10 µM. IPA-3 inhibits the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) endoribonuclease nsp15 in a FRET assay (IC50 = 6.8 µM) and inhibits SARS-CoV-2 replication in infected Vero CCL-81 cells (IC50 = 8.5 µM).2 It inhibits the proliferation of H2M and MHCC97-L metastatic hepatocellular carcinoma (HCC) and non-metastatic HepG2 HCC cells when used at concentrations of 5 and 10 µM. IPA-3 (2 and 4 mg/kg) reduces tumor growth in an MHCC97-L cell mouse xenograft model.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Deacon, S.W., Beeser, A., Fukui, J.A., et alAn isoform-selective, small-molecule inhibitor targets the autoregulatory mechanism of p21-activated kinase. Chem. Biol. 15(4), 322-331 (2008).

    2. Chen, J., Farraj, R.A., Velazquez, D.L., et alReversible and irreversible inhibitors of coronavirus Nsp15 endoribonuclease. The Journal of Biological Chemisty 11, 105341 (2023).

    3. Wong, L.L.-Y., Lam, I.P.-Y., Wong, T.Y.-N., et alIPA-3 inhibits the growth of liver cancer cells by suppressing PAK1 and NF-κB activation. PLoS One 8(7), e68843 (2013).