Lurtotecan (GI147211; OSI-211), a semisynthetic Camptothecin analog, is a topoisomerase I inhibitor. Lurtotecan has anticancer effects.

ZDLD20, a β-carboline, is orally active and selective CDK4/CycD3 inhibitor with an IC50 value of 6.51  μM. ZDLD20 exhibits potent anti-HCT116 activity including inhibition of colony formation, inhibition of invasion and migration, inducing of apoptosis, and arresting of G1 phase in cell cycle. ZDLD20 exhibits potent anticancer activity.

AZD5099, an antibacterial agent, is a potent and selective bacterial topoisomerase II inhibitor. AZD5099 potently inhibits the infections caused by Gram-positive and fastidious Gram-negative bacteria.

Pralatrexate(Folotyn) is an antifolate, and structurally a folate analog.

TDRL-X80 is a potent inhibitor of xeroderma pigmentosum group A (XPA) protein. TDRL-X80 inhibits XPA’s DNA binding activity. TDRL-X80 exhibits activity against single, double, and Cisplatin-damaged DNA with IC50s of 18, 20, and 29 μM in fluorescence polarization (FP) analyses , and with IC50s of 21, 39, and 28 in ELISA Analysis.

AS-136A is an orally active non-nucleoside inhibitor of the measles virus RNA-dependent RNA polymerase (RdRp) with an IC50 of 2 µM for measles virus.

Alatrofloxacin, the parenteral prodrug of Trovafloxacin, is a fluoronaphthyridone which contains an L-alanyl-L-alanyl salt. Alatrofloxacin functions similar to other fluoroquinolone antibiotics in that it not only has antibiotic activity to kill invading organisms by interfering with DNA synthesis, it possesses immunosuppressive activity.

4-Aminonaphthalimide is a potent PARP inhibitor and potentiates the cytotoxicity of γ-radiation in cancer cells.

Quarfloxin (CX-3543) is a fluoroquinolone derivative with antineoplastic activity.

RI-1 is a RAD51 inhibitor with IC50 ranging from 5 to 30 μM.

Roscovitine (Seliciclib, CYC202, R-roscovitine) is a potent and selective CDK inhibitor for Cdc2/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p53 with IC50 of 0.65 μM, 0.7 μM, 0.7 μM and 0.16 μM, respectively.

Rucaparib (AG-014699, PF-01367338) is an inhibitor of PARP with Ki of 1.4 nM with binding affinity to nine PARP domains. Phase 1/2.

Rucaparib inactivates PARP activity in cells with homologous recombination DNA repair pathway mutations at LC50 values ranging from 1.3-5.5 μM.

SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC(50) of 13.3 nmol/L on the isolated human enzyme.

SU-9516 is a selective CDK2 inhibtor with IC50 of 22 nM; less potent for CDK1/CDK4(IC50=40/200 nM), no inhibition on PKC, EGFR, p38MAPK etc.

TAI-1 is a potent and specific Hec1 inhibitor, which disrupts Hec1-Nek2 protein interaction.

TAS-103 2Hcl(BMS-247615 2Hcl) is a dual inhibitor of topoisomerase-I (topo-I) and topoisomerase-II (topoII).

Tipiralacil(TPI) is a thymidine phosphorylase inhibitor (TPI). Tipiracil is one of the active components in TAS-102, which is an anticancer drug candidate currently in clinical trials.

Veliparib (ABT-888) is a potent inhibitor of PARP1 and PARP2 with Ki of 5.2 nM and 2.9 nM, respectively.

Voruciclib is a protein kinase inhibitor specific for the cyclin-dependent kinase 4 (CDK4) with potential antineoplastic activity.

VX-680 (MK-0457, Tozasertib) is a pan-Aurora inhibitor of Aurora A, Aurora B and Aurora C with Kiapp of 0.6 nM, 18 nM and 4.6 nM, respectively.

GSK461364 is a potent small molecule Polo-like kinase 1 (PLK1) inhibitor with a Ki of 2.2 nM.

SPHINX31 is a potent inhibitor of serine/arginine-rich protein kinase 1 (SRPK1; IC50 = 5.9 nM).

Zebularine (NSC309132, 4-Deoxyuridine) is a nucleoside analog of cytidine and inhibitor of cytidine deaminase, also inhibits DNA methylation and tumor growth both in vitro and in vivo.

Wee1 Inhibitor II is a potent, selective, ATP-binding site-targeting inhibitor of Wee1 with IC50 of 59 nM, 590-fold selectivity over the related checkpoint kinase Chk1 (IC50=35 uM).

Thymidine Phosphorylase inhibitor 8g (hTP inhibitor 8g) is a novel potent, selective inhibitor of human thymidine phosphorylase (hTP) with IC50 of 0.12 uM; induces DNA damage measured with the alkaline comet assay in HepG2 cells; hTP inhibitor 8g (50 mg/kg/day) for two weeks (5 days/week) significantly reduced tumor growth using an in vivo glioblastoma model.

TH9028 (TH-9028) is a potent and selective inhibitor of folate metabolism enzyme MTHFD2 with IC50 of 11 nM.TH9028demonstrated efficacy on HL-60 cell viability with EC50 of 11 nM.TH9028 potently inhibits related MTHFD proteins MTHFD2L and MTHFD1-(DC) with IC50 of 47 and 16 nM, respectively.

SY-5102 (SY5102) is a highly potent, selective, noncovalent, orally available CDK7 inhibitor with SPR Kd of 0.03 nM (binding to CDK7/Cyclin H).SY-5102 (SY5102) displays highly selectivity against CDK2, CDK9, and CDK12 (all IC50>75 nM).SY-5102 potently inhibits HCC70 cell proliferation with EC50 of 9 nM.SY-5102 showed dose-dependent tumor growth inhibition including tumor regression at 4 mg/kg po (dosed twice daily) in an HCC70 cell line derived xenograft mouse model.

SCR7 is a specific inhibitor of nonhomologous end-joining (NHEJ), blocks Ligase IV-mediated joining by interfering with its DNA binding but not that of T4 DNA Ligase or Ligase I; inhibits NHEJ in a Ligase IV-dependent manner within cells, causes accumulation of double-strand breaks (DSBs), and activates the intrinsic apoptotic pathway; decreases cell proliferation of MCF7, A549, and HeLa with IC50 of 40, 34, and 44 uM, respectively; increases the efficacy of DSB-inducing therapeutic modalities in mouse xenografts; increases the efficiency of precise genome editing with CRISPR-Cas9 in mammalian cell lines and in mice.

RP12146 (RP12146) is a novel, selective, and potent small molecule inhibitor of PARP1/2 with IC50 of 0.6/0.5 nM, with several fold selectivity over other isoforms.RP12146 inhibited cell growth in both BRCA mutant and non-BRCA mutant cancer cell lines with a GI50 range of 0.043 to 19.83 µM in a dose dependent manner.RP12146 demonstrated anti-tumor activities in both tumor size and tumor weight in OVCAR3 xenograft model.