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Cat. No. Product Name CAS No. Information
PC-61324

HL001

1186371-31-2

HL001 (HL 001) is a potent cyclophilin A (CypA) inhibitor with IC50 of 31.6 nM, induces NSCLC cell cycle arrest and apoptosis via restoring p53 expression; stabilizes p53 through inhibiting the MDM2-mediated p53 ubiquitination, and downregulates G3BP1 and induces ROS and DNA damage; selectively suppresses tumor growth in p53 wild-type NSCLC harboring p53-72R through disrupting interaction between MDM2 and p53-72R in a CypA-dependent manner; synergistically enhance tumor regression in orthotopic NSCLC mouse model combined with cisplatin.

PC-60302

DS-3032b

1398568-47-2

DS-3032b is a potent, selective, orally available MDM2-p53 inhibitor with potential antineoplastic activity; binds to, and prevents the binding of MDM2 protein to the transcriptional activation domain of the tumor suppressor protein p53; restores p53 signaling and leads to the p53-mediated induction of tumor cell apoptosis.

Blood Cancer

Phase 1 Clinical

PC-70003

HDM-201

1448867-41-1

HDM-201 (NVP-HDM 201, Siremadlin) is a highly potent p53-MDM2 interaction inhibitor with biochemical IC50 of 0.13 nM, cellular IC50 of 90 nM; a second generation p53-MDM2 inhibitor that recently entered phase I clinical trial.

PC-45497

NSC-319726

71555-25-4

NSC-319726 (NSC319726) is an allele-specific p53 mutant reactivator; restores WT structure and function to the p53(R175) mutant; kills p53(R172H) knockin mice with extensive apoptosis and inhibits xenograft tumor growth in a 175-allele-specific mutant p53-dependent manner.

PC-45588

SAR-405838

1303607-60-4

SAR-405838(MI-77301, MI-773) is a potent and highly selective small-molecule inhibitor of MDM2-p53 interaction with Ki of 0.88 nM; activates wild-type p53 in vitro and causes p53-dependent cell-cycle arrest and/or apoptosis; shows durable tumor regression or complete tumor growth inhibition in mouse xenograft models of SJSA-1 osteosarcoma, RS4;11 acute leukemia, LNCaP prostate cancer, and HCT-116 colon cancer; orally bioactive.

Blood Cancer

Phase 1 Clinical

PC-35309

MB710

2230044-57-0 MB710 is a small-molecule p53 mutant Y220C stabilizer, binds tightly to the Y220C pocket and stabilizes p53-Y220C in vitro.
PC-35308

MB725

2230058-99-6 MB725 is a small-molecule p53 mutant Y220C stabilizer, induces selective viability reduction in several p53-Y220C cancer cell lines (Huh7 cell IC50=10 uM); reduction of viability correlated with increased and selective transcription of p53 target genes such as BTG2, p21, PUMA, FAS, TNF, and TNFRSF10B, which promote apoptosis and cell cycle arrest, suggesting compound-mediated transcriptional activation of the Y220C mutant.

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