Synthetic Lethality

Cat.No. Product Name Information Product Use Citations Product Validations
S1060 AZD2281 (Olaparib) Olaparib (AZD2281, KU0059436) is a selective inhibitor of PARP1/2 with IC50 of 5 nM/1 nM in cell-free assays, 300-times less effective against tankyrase-1. Olaparib induces significant autophagy that is associated with mitophagy in cells with BRCA mutations.
Cell, 2025, 188(18):5081-5099.e27
Cancer Cell, 2025, 43(8):1530-1548.e9
Cancer Cell, 2025, 43(4):776-796.e14
Verified customer review of AZD2281 (Olaparib)
S7693 Ceralasertib (AZD6738) Ceralasertib (AZD6738) is an orally active and selective ATR kinase inhibitor with IC50 of 1 nM, currently in Phase 1/2 clinical trials.
Cancer Cell, 2025, 43(8):1530-1548.e9
Nat Cell Biol, 2025, 27(1):73-86
Nat Commun, 2025, 16(1):8476
Verified customer review of Ceralasertib (AZD6738)
S7048 BMN-673 (Talazoparib) Talazoparib (BMN 673, LT-673) is a novel PARP inhibitor with IC50 of 0.57 nM for PARP1 in a cell-free assay. It is also a potent inhibitor of PARP-2, but does not inhibit PARG and is highly sensitive to PTEN mutation. Phase 3.
Mol Cancer, 2025, 24(1):217
Nat Commun, 2025, 16(1):8476
Nat Commun, 2025, 16(1):6972
Verified customer review of BMN-673 (Talazoparib)
E1349 TNG908 (Ralometostat) Ralometostat (TNG908) is a potent, selective, and brain-penetrant inhibitor of PRMT5 with an IC50 of 4 μM, acting through an MTA-cooperative mechanism. It also shows antitumor activity in a xenograft model.
S8680 AZD1390 AZD1390 is a first-in-class orally available and CNS penetrant ATM inhibitor with an IC50 of 0.78 nM in cells and >10,000-fold selectivity over closely related members of the PIKK family of enzymes and excellent selectivity across a broad panel of kinases.
Cell Rep Med, 2025, 6(7):102202
iScience, 2025, 28(2):111842
Nature, 2024, 629(8011):443-449
S1180 XAV-939 XAV-939 (NVP-XAV939) selectively inhibits Wnt/β-catenin-mediated transcription through tankyrase1/2 inhibition with IC50 of 11 nM/4 nM in cell-free assays, regulates axin levels and does not affect CRE, NF-κB or TGF-β.
Nat Biotechnol, 2025, 10.1038/s41587-025-02649-1
Nat Cell Biol, 2025, 27(8):1240-1255
Nat Cell Biol, 2025, NONE
Verified customer review of XAV-939
S8664 GSK3326595 (Pemrametostat, EPZ015938) Pemrametostat (GSK3326595, EPZ015938) is an orally active, potent and selective inhibitor of protein arginine methyltransferase 5 (PRMT5) and potently inhibits tumor growth in vitro and in vivo in animal models.
MedComm (2020), 2025, 6(6):e70150
J Med Chem, 2025, 68(4):4217-4236
J Med Chem, 2025, 68(5):5097-5119
E1939 ART899 ART899, a derivative of ART558 is a potent, specific allosteric inhibitor of DNA polymerase theta (Polθ), specifically inhibits Polθ MMEJ activity with IC50 of 180 nM. It specifically radiosensitizes tumor cells and have a potent stand-alone antitumor effect in cancer cells.
S7102 Berzosertib (VE-822) Berzosertib (VE-822, VX970, M6620) is an ATR inhibitor with IC50 of 19 nM in HT29 cells.
Cancer Cell, 2025, 43(8):1530-1548.e9
Nat Cell Biol, 2025, 27(1):59-72
Nat Commun, 2025, 16(1):3613
Verified customer review of Berzosertib (VE-822)
S8883 LLY-283 LLY-283 is a novel and selective inhibitor of protein arginine methyltransferase 5 (PRMT5). This compound inhibits PRMT5 enzymatic activity in vitro and in cells with IC50 of 22 nM and 25 nM, respectively. It shows antitumor activity.
Nucleic Acids Research, 2026, gkag016
Mol Cancer Res, 2025, 23(2):107-118
Res Sq, 2025, rs.3.rs-5936706