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Australia
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United States
Synthetic Lethality Inhibitors
| 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. |
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| S1009 | Dactolisib (BEZ235) | Dactolisib (BEZ235, NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM /5 nM /7 nM /75 nM /6 nM in cell-free assays, respectively. It inhibits ATR with IC50 of 21 nM in 3T3TopBP1-ER cell, induces autophagy, and suppresses HIV-1 replication. Phase 2. |
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| 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. |
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| S1092 | KU-55933 | KU-55933 is a potent and specific ATM inhibitor with IC50/Ki of 12.9 nM/2.2 nM in cell-free assays, and is highly selective for ATM as compared to DNA-PK, PI3K/PI4K, ATR and mTOR. KU‑55933 (ATM Kinase Inhibitor) inhibits the activation of autophagy‑initiating kinase ULK1 and results in a significant decrease of autophagy. |
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| S2913 | BAY 11-7082 (BAY 11-7821) | BAY 11-7082 (BAY 11-7821) is a NF-κB inhibitor, inhibits TNFα-induced IκBα phosphorylation with IC50 of 10 μM in tumor cells. BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 with IC50 of 0.19 μM and 0.96 μM, respectively. BAY 11-7082 induces apoptosis and S phase arrest in gastric cancer cells. |
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| S2758 | Wortmannin (SL-2052) | Wortmannin is the first described PI3K inhibitor with IC50 of 3 nM in a cell-free assay, with little selectivity within the PI3K family. Wortmannin blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays. Wortmannin also inhibits PLK1 activity. |
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| 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. |
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| S8007 | VE-821 | VE-821(ATR inhibitor IV) is a potent and selective ATP competitive inhibitor of ATR with Ki/IC50 of 13 nM/26 nM in cell-free assays, shows inhibition of H2AX phosphorylation, minimal activity against PIKKs ATM, DNA-PK, mTOR and PI3Kγ. |
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| S1004 | Veliparib (ABT-888) | Veliparib (ABT-888, NSC 737664) is a potent inhibitor of PARP1 and PARP2 with Ki of 5.2 nM and 2.9 nM in cell-free assays, respectively. This compound is inactive to SIRT2 and increases autophagy and apoptosis. Phase 3. |
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| S1525 | Adavosertib (AZD1775, MK-1775) | Adavosertib (MK-1775, AZD1775) is a potent and selective Wee1 inhibitor with IC50 of 5.2 nM in a cell-free assay; hinders G2 DNA damage checkpoint. Phase 2. |
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| S4157 | Chloroquine diphosphate | Chloroquine diphosphate is a 4-aminoquinoline anti-malarial and anti-rheumatoid agent, also acting as an ATM activator. Chloroquine is also an inhibitor of toll-like receptors (TLRs). |
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| S1570 | KU-60019 | KU-60019 is an improved analogue of KU-55933, with IC50 of 6.3 nM for ATM in cell-free assays, 270- and 1600-fold more selective for ATM than DNA-PK and ATR,and is a highly effective radiosensitizer. |
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| 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. |
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| S7102 | Berzosertib (VE-822) | Berzosertib (VE-822, VX970, M6620) is an ATR inhibitor with IC50 of 19 nM in HT29 cells. |
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| S1098 | Rucaparib phosphate | Rucaparib phosphate is an inhibitor of PARP with Ki of 1.4 nM for PARP1 in a cell-free assay, also showing binding affinity to eight other PARP domains. Phase 3. |
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| S2741 | Niraparib (MK-4827) | Niraparib (MK-4827) is a selective inhibitor of PARP1/2 with IC50 of 3.8 nM/2.1 nM, with great activity in cancer cells with mutant BRCA-1 and BRCA-2. It is >330-fold selective against PARP3, V-PARP and Tank1. This compound can form PARP–DNA complexes resulting in DNA damage, apoptosis, and cell death. Phase 3. |
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| S2817 | Torin 2 | Torin 2 is a potent and selective mTOR inhibitor with IC50 of 0.25 nM in p53−/− MEFs cell line; 800-fold greater selectivity for mTOR than PI3K and improved pharmacokinetic properties. This compound inhibits ATM/ATR/DNA-PK with EC50 of 28 nM/35 nM/118 nM,in PC3 cell lines respectively. It decreases cell viability and induces autophagy and apoptosis. |
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| S4948 | Rucaparib (AG-014699) | Rucaparib is an inhibitor of PARP with Ki of 1.4 nM for PARP1 in a cell-free assay, also showing binding affinity to eight other PARP domains. |
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| S7050 | AZ20 | AZ20 is a novel potent and selective inhibitor of ATR kinase with IC50 of 5 nM in a cell-free assay, 8-fold selectivity over mTOR. |
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| S2243 | Degrasyn (WP1130) | Degrasyn (WP1130) is a selective deubiquitinase (DUB: USP5, UCH-L1, USP9x, USP14, and UCH37) inhibitor and also suppresses Bcr/Abl, also a JAK2 transducer (without affecting 20S proteasome) and activator of transcription (STAT). This compound induces apoptosis and blocks autophagy. |
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| S8375 | AZD0156 | AZD0156 is a potent and selective inhibitors of ATM kinase, with potential chemo-/radio-sensitizing and antineoplastic activities. AZD0156 prevents DNA damage checkpoint activation, disrupts DNA damage repair, induces tumor cell apoptosis, and leads to cell death of ATM-overexpressing tumor cells. |
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| S7300 | PJ34 HCl | PJ34 HCl is the hydrochloride salt of PJ34, which is a PARP inhibitor with EC50 of 20 nM and is equally potent to PARP1/2. |
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| S7888 | Spautin-1 | Spautin-1 is a potent and specific autophagy inhibitor, and inhibits the deubiquitinating activity of USP10 and USP13 with IC50 of ∼0.6-0.7 μM. This compound enhances apoptosis. |
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| S7625 | Niraparib tosylate | Niraparib tosylate is a selective inhibitor of PARP1/PARP2 with IC50 of 3.8 nM/2.1 nM. Niraparib increases formation of PARP-DNA complexes resulting in DNA damage, apoptosis, and cell death. |
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| S2178 | AG-14361 | AG14361 is a potent inhibitor of PARP1 with Ki of <5 nM in a cell-free assay. It is at least 1000-fold more potent than the benzamides. |
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| S8096 | Mirin | Mirin is a potent Mre11–Rad50–Nbs1 (MRN) complex inhibitor, and inhibits Mre11-associated exonuclease activity. This compound inhibits MRN-dependent activation of ATM. |
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| S7748 | EPZ015666 (GSK3235025) | EPZ015666 (GSK3235025) is a potent, selective and orally bioavailable PRMT5 inhibitor with Ki of 5 nM, >20,000-fold selectivity over other PMTs. |
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| 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. |
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| S7134 | IU1 | IU1 is a cell-permeable, reversible and selective proteasome inhibitor of human USP14 with IC50 of 4.7 μ M, 25-fold selective to IsoT. This compound induces autophagy. |
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| 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. |
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| S7529 | ML323 | ML323 displays reversible, nanomolar inhibitory activity and excellent selectivity toward USP1/UAF1 with IC50 of 76 nM. |
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| S1087 | Iniparib (BSI-201) | Iniparib (BSI-201, NSC-746045, IND-71677) is a PARP1 inhibitor with demonstrated effectiveness in triple-negative breast cancer (TNBC). Phase 3. |
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| S5195 | Rucaparib Camsylate | Rucaparib (Rubraca, AG014699, PF01367338) Camsylate is an inhibitor of PARP with Ki of 1.4 nM for PARP1 in a cell-free assay, also showing binding affinity to eight other PARP domains. |
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| S2245 | CP-466722 | CP-466722 is a potent and reversible ATM inhibitor, does not affect ATR and inhibits PI3K or PIKK family members in cells. |
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| S9864 | Elimusertib (BAY 1895344) | Elimusertib (BAY-1895344) is a very potent and highly selective ATR (ataxia telangiectasia and Rad3-related) inhibitor with IC50 of 7 nM. Elimusertib potently inhibits proliferation of a broad spectrum of human tumor cell lines with median IC50 of 78 nM. |
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| S7239 | G007-LK | G007-LK is a potent and selective tankyrase inhibitor with IC50 of 46 nM and 25 nM for TNKS1/2, respectively. |
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| S2197 | A-966492 | A-966492 is a novel and potent inhibitor of PARP1 and PARP2 with Ki of 1 nM and 1.5 nM, respectively. |
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| S8050 | ETP-46464 | ETP-46464 is a potent and selective inhibitor of ATR with IC50 of 25 nM. |
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| S8592 | Pamiparib | Pamiparib is a potent and selective inhibitor of PARP1 and PARP2 with IC50 values of 0.83 and 0.11 nM, respectively in biochemical assays. It shows high selectivity over other PARP enzymes. |
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| S8038 | UPF 1069 | UPF 1069 is a selective PARP2 inhibitor with IC50 of 0.3 μM. It is ~27-fold selective against PARP1. |
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| S8363 | NMS-P118 | NMS-P118 is a potent, orally available, and highly selective PARP-1 inhibitor endowed with excellent ADME and pharmacokinetic profiles, showing 150-fold selectivity for PARP-1 over PARP-2 (Kd 0.009 μM vs 1.39 μM, respectively). |
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| S8419 | Stenoparib (E7449) | Stenoparib (E7449, 2X-121, MGI25036) is an orally bioavailable, brain penetrable, small molecule dual inhibitor of PARP1/2 and also inhibits PARP5a/5b, otherwise known as tankyrase1 and 2 (TNKS1/2), important regulators of canonical Wnt/β-catenin signaling. It has IC50 values of 1.0 and 1.2 nM for PARP1 and 2, respectively. |
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| S8148 | PD0166285 | PD0166285 is a potent Wee1 and Chk1 inhibitor with activity at nanomolar concentrations (IC50=24 nM for Wee1 and 72 nM for Myt1). This compound is also a novel G2 checkpoint abrogator. It induces apoptosis. |
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| S9639 | VX-803 (M4344) | VX-803 (M4344, ATR inhibitor 2) is an ATP-competitive, orally active, and selective inhibitor of ataxia telangiectasia and Rad3 related (ATR) kinase with Ki of < 150 pM. This compound potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (P-Chk1) phosphorylation with IC50 of 8 nM. It exhibits potential antineoplastic activity. |
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| S7029 | AZD2461 | AZD2461 is a novel PARP inhibitor with low affinity for Pgp. Phase 1. |
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| S7438 | ME0328 | ME0328 is a potent and selective PARP inhibitor with IC50 of 0.89 μM for PARP3, about 7-fold selectivity over PARP1. |
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| S8370 | BGP-15 2HCl | BGP-15, is a nicotinic amidoxime derivative with PARP inhibitory activity. It has been demonstrated that BGP-15 protects against ischemia-reperfusion injury. |
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| S8624 | Onametostat (JNJ-64619178) | Onametostat (JNJ-64619178) is a PRMT5 inhibitor with high selectivity and potency (subnanomolar range, PRMT5-MEP-50 IC50=0.14 nM) under different in vitro and cellular conditions, paired with favorable pharmacokinetics and safety properties. |
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| S1132 | 3-Aminobenzamide | 3-Aminobenzamide (3-ABA , 3-Amino Benzamide, 3-AB) is a potent inhibitor of Poly(ADP-ribose)polymerase (PARP) and inhibits cell apoptosis after SCI (Spinal Cord Injury) in caspase-independent way. |
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| S9875 | AZD5305 (Saruparib) | Saruparib (AZD5305) is a highly selective and potent inhibitor of PARP1 with an IC50 of 3 nM in wild-type A549 lung cancer cells. AZD5305 shows no or minimal growth inhibitory effects in other cells (IC50s >10μM). |
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| S7238 | NVP-TNKS656 | NVP-TNKS656 is a highly potent, selective, and orally active tankyrase inhibitor with IC50 of 6 nM for TNKS2, > 300-fold selectivity against PARP1 and PARP2. |
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| S0435 | PF-9366 | PF-9366 is a human methionine adenosyltransferase 2A (MAT2A) inhibitor with IC50 of 420 nM and Kd of 170 nM. |
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| S7136 | CGK 733 | CGK 733 is a potent and selective inhibitor of ATM/ATR with IC50 of ~200 nM. |
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| S7730 | NU1025 | NU1025 (NSC 696807) is a potent PARP inhibitor with IC50 of 400 nM. |
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| E1175 | RP-6306 (lunresertib) | lunresertib (RP-6306) is a Protein Kinase, Membrane Associated Tyrosine/Threonine 1 (PKMYT1) inhibitor, which can be used for the research of cancer. |
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| S9936 | ART558 | ART558 is a potent, selective, low molecular weight, allosteric inhibitor of DNA Polθ with an IC50 of 7.9 nM. |
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| E1024 | MRTX1719 (Navlimetostat) | MRTX1719 is a potent, selective inhibitor of the protein arginine methyltransferase 5·methylthioadenosine phosphorylase complex (PRMT5•MTA), a potentially tumor-selective target for therapeutic intervention. |
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| S4715 | Benzamide | Benzamide, a derivative of benzoic acid, is an inhibitor of poly(ADP-ribose) polymerase with an IC50 of 3.3 μM. |
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| S8556 | AZ31 | AZ31 is a selective and novel ATM inhibitor with an IC50 of <0.0012 μM. It shows excellent selectivity over closely related enzymes (>500 fold selective over DNA-PK and PI3Kα and >1000 fold selective over mTOR, PI3Kβ and PI3Kγ). |
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| S0399 | SJB2-043 | SJB2-043 is a potent USP1 inhibitor that inhibits the activity of native USP1/UAF1 with IC50 of 544 nM. |
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| S2837 | BCI chemical | BCI ((E)-BCI, compound 1) is an allosteric dual specificity phosphatase (DUSP) inhibitor with EC50 of 13.3 μM and 8.0 μM in cells for DUSP6 and DUSP1, respectively. |
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| S8209 | HLCL-61 HCL | HLCL-61 hydrochloride is a potent and selective PRMT5 inhibitor for the treatment of acute myeloid leukemia. |
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| S7490 | WIKI4 | WIKI4 is a novel Tankyrase inhibitor with IC50 of 15 nM for TNKS2, and leads to inhibition of Wnt/beta-catenin signaling. |
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| S6745 | JW55 | JW55 is a potent and selective inhibitor of the canonical Wnt pathway that functions via inhibition of the PARP domain of tankyrase 1 and tankyrase 2 (TNKS1/2). |
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| E1479 | I-138 | I-138 is an orally active, potent reversible inhibitor of USP1-UAF1 with IC50 0f 4.1 nM. This compound is structurally related to ML323 and induces the monoubiquitination of FANCD2 and PCNA in MDA-MB-436 cells and increases PCNA and FANCD2 monoubiquitination in HAP-1 USP1 WT cells. |
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| E1528 | RP-6685 | RP-6685 is a potent, selective, and orally active inhibitor of DNA polymerase theta (Polθ). RP-6685 exhibits antitumor efficacy in animal models. |
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| S8993 | Atamparib (RBN-2397) | RBN-2397 (Atamparib) is a potent, selective and orally active NAD+ competitive inhibitor PARP7 with IC50 of <3 nM and Kd of <0.001 μM. This compound has the potential for the research of tumor treatment. |
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| S9778 | Zedoresertib (Debio-0123, WEE1-IN-5) | WEE1-IN-5 (Debio 0123) is a potent Wee1 inhibitor that inhibits phospho-CDC2 and abrogates the G2 check point. |
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| S8729 | AZ32 | AZ32 is a specific inhibitor of the ATM kinase that possesses good BBB penetration in mouse with an IC50 value of <0.0062 μM for ATM enzyme. It shows adequate selectivity over ATR and also has high cell permeability. |
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| S9712 | Fluzoparib (SHR-3162) |
Fluzoparib (SHR3162, HS10160) is a potent Poly (ADP-ribose) polymerase (PARP) inhibitor that shows anti-tumor activity, with an IC50 of 1.46±0.72 nM for PARP1. |
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| E1000 | Azenosertib (Zn-C3) | Azenosertib (Zn-C3) is an oral active, highly effective and selective Wee1 inhibitor with IC50 of 3.9 nM, which can be used in cancer research. |
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| S0148 | HAMNO | HAMNO (NSC-111847) is a potent and selective replication protein A (RPA) inhibitor with anti-tumor activity. This compound inhibits both ATR autophosphorylation and phosphorylation of RPA32 Ser33 by ATR. |
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| S6885 | Ailanthone | Ailanthone (AIL, Δ13-Dehydrochaparrinone), a natural anti-hepatocellular carcinoma (HCC) component in Ailanthus altissima, induces G0/G1-phase cell cycle arrest by decreasing expression of cyclins and CDKs and increases expression of p21 and p27. This compound triggers DNA damage characterized by activation of the ATM/ATR pathway. It induces apoptosis which is mitochondrion-mediated and involves the PI3K/AKT signaling pathway in Huh7 cells. This chemical is also a potent inhibitor of both full-length Androgen Receptor (AR-FL) and constitutively active truncated AR splice variants (AR-Vs, AR1-651) with IC50 of 69 nM and 309 nM, respectively. |
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| E1057 | Lartesertib (M4076) | Lartesertib (M4076) inhibits Ataxia telangiectasia-mutated (ATM) kinase activity with a sub-nanomolar potency and shows remarkable selectivity against other protein kinases, suppresses DSB repair, clonogenic cancer cell growth, and potentiates antitumor activity of ionizing radiation in cancer cell lines. |
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| S8992 | RBN012759 | RBN012759 is a potent and selective inhibitor of PARP14 with IC50 of <3 nM and 5 nM for human catalytic domain and mouse catalytic domain, respectively. This compound contributes to anti-tumor immune response. |
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| E1214 | KSQ-4279 (USP1-IN-1) | KSQ-4279 (USP1-IN-1) is an orally bioavailable selective inhibitor of the ubiquitin specific protease 1 (USP1) with anti-proliferative activity. KSQ-4279 also exhibits synergistic activity in combination with PARP inhibitors. |
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| S0519 | BYK204165 | BYK204165 is a potent and selective inhibitor of the poly(ADP-ribose) polymerase (PARP). This compound inhibits cell-free recombinant human PARP-1 (hPARP-1) with pIC50 of 7.35 and pKi of 7.05 and murine PARP-2 (mPARP-2) with pIC50 of 5.38, respectively. |
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| E0111 | BRM/BRG1 ATP Inhibitor-1 (BRM014) | BRM/BRG1 ATP Inhibitor-1 (Compound 14) is an orally active inhibitors of Brahma Homolog (BRM)/SMARCA2 (BRG1) with IC50s below 0.005 µM. |
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| E2147 | AZD9574 (Palacaparib) | AZD9574 is a novel PARP inhibitor which combines PARP1 selectivity, trapping and high CNS penetration in a single molecule. |
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| S4710 | Picolinamide | Picolinamide (2-Pyridinecarboxamide, Picolinoylamide, 2-Carbamoylpyridine) is found to be a strong inhibitor of poly (ADP-ribose) synthetase of nuclei from rat pancreatic islet cells. |
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| E1425 | Nesuparib | Nesuparib (JPI-547, NOV140201) is a potential inhibitor of both PARP and tankyrases, with IC50 of 0.005 μM, 0.001 μM, 0.002 μM, and ND for TNKS1, TNKS2, PARP1, and PARP2, respectively. This compound exhibits anti-tumor activity in BRCA-deficient xenograft models. | ||
| S6899 | Licochalcone D | Licochalcone D (Lico D, LCD, LD), a flavonoid isolated from a Chinese medicinal plant Glycyrrhiza inflata, has antioxidant, anti-inflammatory and anti-cancer properties. This compound inhibits phosphorylation of NF-κB p65 in LPS signaling pathway. It inhibits JAK2, EGFR and Met (c-Met) activities and induces ROS-dependent apoptosis. This chemical also induces caspases activation and poly (ADP-ribose) polymerase (PARP) cleavage. | ||
| E1411 | Tuvusertib | Tuvusertib (M1774, ATR inhibitor 1) is a potent ATR inhibitor, which exhibits anti-proliferative and anti-tumor effects in cancer cell lines. | ||
| S6977 | DR2313 | DR2313 is a potent, selective, competitive and brain-penetrant inhibitor of poly(ADP-ribose) polymerase (PARP), with IC50s of 0.20 μM and 0.24 μM for PARP-1 and PARP-2, respectively. | ||
| S6739 | MN 64 | MN-64 is a potent inhibitor of TNKS1 and TNKS2 with IC50 value of 6 and 72 nM, respectively. | ||
| E1007 | BRD0639 |
BRD0639 is a first-in-class PBM-competitive small molecule inhibitor that disrupts the PRMT5-RIOK1 complex with IC50s of 7.5 μM and 16 μM in permeabilized and living cells, respectively. |
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| E1069 | M2912 | M2912 (MSC2504877) is a very potent TNKS1/TNKS2 inhibitor (IC50=0.6 nM for TNKS1) with exquisite selectivity over other PARP family enzymes and favorable compound properties. This inhibitor potently modulates the Wnt/β-catenin pathway by elevating the levels of axin2 (EC50=17 nM) and tankyrase in DLD1 cells in a dose-dependent manner resulting in reduced cellular Wnt reporter activity. | ||
| E5945New | Wu-5 | Wu-5 is an inhibitor of USP10 that blocks its activity in vitro with an IC50 of 8.3 µM. It also promotes FLT3-ITD degradation and synergistically enhances crenolanib-induced apoptosis. | ||
| S0732 | GeA-69 | GeA-69 is a cell-permeable, selective allosteric inhibitor targeting macrodomain 2 (MD2) of poly-adenosine-diphosphate-ribose polymerase 14 (PARP14) with Kd of 860 nM. | ||
| E1108 | Camonsertib (RP-3500) | Camonsertib (RP-3500) is a highly potent and selective inhibitor of ATR kinase with an IC50 of 1 nM. | ||
| E8297New | Myt1-IN-1 | Myt1-IN-1 is a potent and selective inhibitor of membrane-associated tyrosine and threonine-specific cdc2-inhibitory kinase (Myt1)(Gene: PKMYT1) with an IC50 of <10 nM. It exhibits anticancer activity and can be used in research on cancers with CCNE1 amplification or FBXW7 mutations that rely on Myt1 activity. | ||
| E1908 | HRO761 | HRO761 is a potent, selective, allosteric inhibitor of Werner syndrome RecQ helicase (WRN). It binds at the interface of the D1 and D2 helicase domains, locking WRN in an inactive conformation, and demonstrates anti-proliferative effects specifically in microsatellite instability (MSI) cancer cells. | ||
| E1614 | OUL232 | OUL232 (Compound 27) is an potent inhibitor of mono-ADP-ribosylation (mono-ARTs) PARP10 with IC50 of 7.8 nM. It also inhibits PARP7, PARP11, PARP12, PARP14, and PARP15 at nM potencies. | ||
| S9893 | Venadaparib(IDX-1197) | Venadaparib (IDX-1197), a potent PARP1/2 inhibitor with IC50 values of 1.4 nM and 1.0 nM respectively, prevents the repair of DNA single-strand breaks (SSB) and promotes the conversion of SSB to double-stranded breaks (DSB), which ultimately leads to synthetic lethality in cancer cells. | ||
| S0056 | (E/Z)-BCI | (E/Z)-BCI (BCI, NSC 150117) is an inhibitor of dual specific phosphatase 1/6 (DUSP1/DUSP6) and mitogen-activated protein kinase with EC50 of 13.3 μM and 8.0 μM for DUSP6 and DUSP1 in cells, respectively. (E)-BCI induces apoptosis via generation of reactive oxygen species (ROS) and activation of intrinsic mitochondrial pathway in H1299 lung cancer cells. | ||
| S8479 | LLY-284 | LLY-284 is the diastereomer of LLY-283, which is a potent and selective SAM-competitive chemical probe for PRMT5. This compound is much less active than LLY-283 and can be used as a negative control for it. | ||
| E1871 | TNG-462 | TNG-462 is an orally active, potent and selective inhibitor of methylthioadenosine (MTA)-cooperative PRMT5. It exhibits significant antitumor activity, including durable regressions and complete responses, against methylthioadenosine phosphorylase (MTAP) deficiency and/or methylthioadenosine (MTA) accumulation solid tumors. | ||
| E1600 | AMG 193 | AMG-193 is an orally active and MTA-cooperative inhibitor of PRMT5 with potent biochemical and cellular activity. AMG-193, in combination with MTA, selectively targets and inhibits the growth of MTAP-deficient tumor cells by suppressing PRMT5, with an IC50 of 0.107 μM, while sparing normal cells that possess wild-type MTAP. AMG-193 also exhibits antitumor activity. | ||
| E4942New | Talazoparib tosylate | Talazoparib tosylate (BMN 673ts) is a potent, orally bioavailable PARP1/2 inhibitor exhibiting an IC50 of 0.57 nM against PARP1. | ||
| S6882 | HI-TOPK-032 | HI-TOPK-032 is a potent and specific inhibitor of TOPK. This compound also reduces ERK-RSK phosphorylation, regulates of the abundance of p53, cleaved caspase-7, and cleaved PARP, and induces apoptosis in cancer cells. | ||
| E4869 | Niraparib hydrochloride | Niraparib hydrochloride (MK-4827 hydrochloride) is a potent poly(ADP-ribose)polymerase (PARP) inhibitor with IC50s of 3.8 and 2.1 nM against both the PARP-1 and PARP-2 enzymes, respectively.It inhibits the repair of radiation-induced DNA double-strand breaks, activates apoptosis, and exhibits anti-tumor activity. | ||
| E0636 | GSK-1520489A | GSK-1520489A(EX-A5430) is an active Protein Kinase, Membrane Associated Tyrosine/Threonine 1 (PKMYT1) inhibitor. | ||
| E1955New | TNG348 | TNG348 is an orally bioavailable allosteric inhibitor targeting the ubiquitin-specific protease USP1. It selectively and potently blocks USP1 activity, preventing deubiquitination of proliferative PCNA and FANCD2, which disrupts DNA repair mechanisms. TNG348 demonstrates inhibitory effects against BRCA1/2-mutated and homologous recombination-deficient (HRD) breast and ovarian cancers . | ||
| E0947 | Iu1-248 | Iu1-248, a derivative of IU1, is a potent and selective ubiquitin specific peptidase 14 (USP14) inhibitor with an IC50 of 0.83 μM. | ||
| E1118New | SJB3-019A | SJB3-019A is a potent inhibitor of USP1 that significantly suppresses cell proliferation and induces apoptosis in B-cell acute lymphoblastic leukemia (B-ALL) cells. It also promotes DNA-binding-1 (ID1) degradation in K562 cells. | ||
| E4719 | XYL-1 | XYL-1 is a highly potent inhibitor of PARP7 with and IC50 of 0.6 nM. It could enhance the type-Ⅰinterferon signaling in vitro, and can be a potential candidate for developing cancer immunotherapy agents. | ||
| E1481New | AM-9747 | AM-9747 (PRMT5-IN-25) is a potent inhibitor of PRMT5 with a Ki of 0.06 nM. It exhibits antiproliferative activity and a significant oral antitumor effect in mouse models employing patient-derived xenografts (PDX). | ||
| E7366 | Veliparib dihydrochloride | Veliparib dihydrochloride is an orally active and potent inhibitor of both PARP-1 and PARP-2 with Kis of 5.2 nM and 2.9 nM, respectively. It exhibit ability to cross the blood-brain barrier and potentiate DNA-damaging agents in preclinical tumor model. | ||
| E1529 | ART812 | ART812 is an orally active DNA polymerase Polθ inhibitor with an IC50 value of 7.6 nM. | ||
| E1989 | ART0380 (Alnodesertib) | ART0380 (IACS-030380) is a potent and selective, orally bioavailable inhibitor of ATR kinase, with an IC50 of 51.7 nM effectively inhibiting the enzyme activity of the ATR-ATRIP complex. It functions as an ATP-competitive inhibitor, binding to the ATP pocket of ATR, where ATP would typically bind. It interacts with the hinge through its morpholine oxygen and occupies the ribose pocket with a sulfoximine group. It also exhibits antitumor activity. | ||
| E1518 | DPQ | DPQ is a potent inhibitor of Poly (ADP-ribose) polymerase (PARP), with an IC50 of 40 nM for PARP1. It also suppresses macrophage-mediated inflammation and mitigates acute lung injury (ALI) induced by lipopolysaccharide (LPS) challenge in mice. | ||
| E1806 | AGI-24512 | AGI-24512 is an inhibitor of MAT2A with an IC50 of 8 nM. It increases R-Loop formation and DNA damage in MTAP-deleted and WT cell models. It also exhibits anti-proliferative activity in vitro. | ||
| S6943 | IU1-47 | IU1-47 is a potent and specific inhibitor of USP14 with an IC50 of 0.6 μM. This compound shows ∼33-fold selectivity for USP14 over USP5 (IsoT). | ||
| S8876 | RK-287107 | RK-287107 is a novel, potent and selective tankyrase inhibitor with antitumor activity. This compound inhibits tankyrase-1 and tankyrase-2 in vitro with IC50 of 14.3 nM and 10.6 nM. | ||
| E7768 | C527 | C527 is a is a pan DUB enzyme inhibitor, with a high potency for the USP1/UAF1 complex (IC50=0.88 μM). | ||
| E1512 | M3541 | M3541 is a potent and selective inhibitor of ATM kinase activity with an IC50 value of 0.25 nM in cell-free assays. This compound suppresses double-strand breaks (DSB) repair, clonogenic cancer cell growth and potentiates antitumor activity of ionizing radiation in cancer cell lines. | ||
| E4701 | CMP-5 | CMP5 is a potent and selective small molecule inhibitor of PRMT5. It is found to selectively block S2Me-H4R3 by inhibiting PRMT5 methyltransferase activity on histone preparations. It also exhibit potential for research into treatment for EBV+ lymphomas and other B-cell NHL subtypes. | ||
| E6541New | PolQi2 | PolQi2 is a PolΘ inhibitor that specifically targets the N-terminal helicase domain of PolΘ, thereby suppressing alt-EJ (alternative end-joining) repair. This compound improves the accuracy and integration efficiency of gene editing across multiple loci and diverse cell lines. Additionally, PolQi2 demonstrates synergistic effects with DNA-PK inhibitors in reducing Cas9-mediated off-target activity. Its application is suitable for gene editing studies. | ||
| E4737 | Potrasertib | Potrasertib (IMP7068, WEE1-IN-10) is a potent and selective inhibitor of WEE1 Kinase. It displays antitumor activity and is well-tolerated in patients with advanced solid tumors. | ||
| 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. | ||
| E1658 | PRT543 | PRT543 is a potent and selective inhibitor of protein arginine methyltransferase 5 (PRMT5) with broad antitumor activity in vitro and in vivo. It also inhibits the methyltransferase activity of the PRMT5/MEP50 complex with an IC50 of 10.8 nM. | ||
| 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. | ||
| S9872 | AG-270 | AG-270 is a potent and non-competitive methionine adenosyltransferase 2A (MAT2A) inhibitor which lessens the intracellular SAM levels and MTAP-null–selective antiproliferative activity. | ||
| E1711 | FHT-1015 | FHT-1015 is a potent, small-molecule, allosteric inhibitor of SMARCA4/SMARCA2 ATPase with IC50 values ≤10 nM. FHT-1205 decreases PD1+TIM3+ cells and cytokine expression in vivo. |
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