DATASHEET
Formulation
Powder
Storage:
Store in dry, dark place at -20C for 1 year.
Product Information:
Molecular Weight: 348.22
Formula: C12 H7 Cl2 N O3 S2
CAS Number: 882257-11-6
InChi Key: LKZLGMAAKNEGCH-UHFFFAOYSA-N
InChi: InChI=1S/C12H7Cl2NO3S2/c1-6(16)10-5-8(15(17)18)12(20-10)19-9-4-2-3-7(13)11(9)14/h2-5H,1H3
Smiles: CC(=O)C1=CC(=C(SC2C=CC=C(Cl)C=2Cl)S1)[N+]([O-])=O
Purity: 98.0
Solubility: DMSO up to 100 mM
Appearance: Solid Power.
Shelf Life: 1.0 years
Description:
P5091 (P005091) is a novel potent and selective inhibitor of ubiquitin-specific protease 7 (USP7) with an IC50 ~4.2 μM. It does not inhibit other DUBs or other families of cysteine proteases tested (EC50 > 100 mM). It induces apoptosis in MM cells resistant to conventional and bortezomib therapies. Biochemical and genetic studies showed that blockade of HDM2 and p21 abrogated P5091-induced cytotoxicity. In animal tumor model studies, P5091 was well tolerated, and it inhibited tumor growth, and prolongs survival. Combining P5091 with lenalidomide, HDAC inhibitor SAHA, or dexamethasone triggered synergistic anti-MM activity.