QBS10072S is a novel dual-function, BBB permeable chemotherapeutic agent with alkylating moiety and a selective large neutral amino acid transporter 1 (LAT1, SLC7A5) substrate, shows excellent BBB penetration and promising efficacy in vitro (U251 cell IC5

ML315 is a small molecule inhibitor of the cdc2-like (Clk) and dual specificity tyrosine phosphorylation-regulated (Dyrk) kinases with IC50 of 68, 231, >10,000, 68, 282 and 1156 nM for CLK1/2/3/4 and DYRK1/2, respectively.

OUL232 is a potent inhibitor of mono-ARTs PARP7, PARP10, PARP11, PARP12, PARP14, and PARP15. OUL232 is the most potent PARP10 inhibitor described to date (IC50=7.8 nM), as well as the first PARP12 inhibitor ever reported.

OUL35 (NSC39047) is a potent and selective inhibitor of mono-ADP-ribosyltransferase PARP10/ARTD10 with IC50 of 330 nM, displays remarkable selectivity towards ARTD10 over other enzymes in the human protein family.

Aurora kinase inhibitor-2 is a selective and ATP-competitive Aurora kinase inhibitor with IC50s of 310 nM and 240 nM for Aurora A and Aurora B, respectively.

GFH009 is a potent, selective CDK9 inhibitor, inhibits the activity of the CDK9/cyclin T1 regulatory complex of P-TEFb.

HRO761 is a potent, selective, allosteric WRN inhibitor with IC50 of 100 nM (ATPase assay) and GI50 of 40 nM (SW48 cells), respectively. HRO761 binds at the interface of the D1 and D2 helicase domains, locking WRN in an inactive conformation.

Treosulfan (NSC 39069, Treosulphan) is an alkylating agent used for conventional and high-dose chemotherapy regimens. Treosulfan is potently cytotoxic against pancreatic cancer cell lines.

DI-87 ((R)-DI-87) is a highly potent, specific, orally bioavailable deoxycytidine kinase (dCK) inhibitor with IC50 of 3.15 nM.

PF-03758309 is an orally bioavailable small-molecule inhibitor of p21-activated kinase 4 (PAK4) with potential antineoplastic activity.

CFI-400945 is a potent, highly selective PLK4 inhibitor with Ki of 0.26 nM and IC50 of 2.8 nM, does not significantly inhibits PLK1/2/3 at 50 uM; causes dysregulated centriole duplication, mitotic defects, and cell death in multiple cancer cell lines (A549 GI50=5 nM, OVCAR-3 GI50=18 nM); significantly inhibits human cancer xenografts; causes polyploidy, growth inhibition, and apoptotic death of murine and human lung cancer cells, despite expression of mutated KRAS or p53, produces supernumerary centrosomes and mitotic defects in lung cancer cells.

PF-07220060 is a potent CDK4/CDK6 inhibitor with a Ki of 0.6 nM and 13.9 nM for CDK4/Cyclin D1 and CDK6/Cyclin D3, respectively.

Nedisertib (M3814, MSC2490484A) is a highly potent, selective, orally bioavailable inhibitor of DNA-PK.

LY2606368 is a potent and selective ATP competitive inhibitor(IC50=1.5 nM in SW1990 cell) of the Chk1 protein kinase.

Votoplam is a gene splicing modulator, used to inhibit Huntington's disease.

Tibremciclib is a CDK4 inhibitor with antineoplastic activity.

LY2880070 is an orally active inhibitor of CHK1. LY2880070 can be used as an anticancer agent and shows promise in preclinical models of pancreatic ductal adenocarcinoma (PDAC) when used in combination with DNA-damaging agents.

LMP744 (MJ-III-65, NSC706744) is a small molecule TOP1 inhibitor antitumoral activity.

Teloxantron (Telomerase inhibitor TXT4) is a potent small molecule inhibitor of telomerase activity with IC50 of 9.61 uM, 7-fold lower than BIBR1532 (Cat# PC-45170), inhibits the processivity of telomerase with preferential DNA damage on telomeres.

DIZ-3 is a dimeric aryl-substituted imidazole as a selective multimeric G-quadruplex (G4) ligand, intercalates into the G4-G4 interface, induces cell cycle arrest and apoptosis, and inhibits cell proliferation in alternative lengthening of telomere (ALT)

Netarsudil (AR-13324) is a potent, selective ROCK inhibitor with Ki of 4.2 nM for ROCK2.

ITRI-E-(S)4046 (E(S)4046) is a potent, highly specific, dual synergistic inhibitor of myosin light chain kinase 4 (MYLK4) and Rho-related protein kinase (ROCK) with IC50 of 3.2 nM and 25.6 nM for ROCK1 and MYLK4, respectively.

C3TD879 is a potent, selective first-in-class Citron kinase (CITK) chemical inhibitor with biochemical IC50 of 12 nM.

(S)-BA-1049 is a potent, orally-available ROCK2-selective inhibitor with IC50 of 0.24 uM, 16-fold selectivity over ROCK-1.

(R)-BA-1049 is a potent, orally-available ROCK2-selective inhibitor with IC50 of 0.24 uM, 16-fold selectivity over ROCK-1.

PLK1 inhibitor SBE13 is a potent, selective PLK1 inhibitor with IC50 of 0.2 nM, with little to no inhibition against PLK2/PLK3 (IC50, 65 uM/875 nM).

HC-5404 (LY-4) is a potent, selective and orally active inhibitor of PKR-like endoplasmic reticulum kinase (PERK, EIF2AK3) with IC50 of 1 nM.

Morataprib Plus is a novel anticancer small molecule that disrupts mortalin-p53 interaction, prevents the interaction of mortalin with p53 resulting in the activation of growth arrest and apoptosis mediated by activation of p21WAF1 or BAX and PUMA signall

Mortaparib is a dual inhibitor of mortalin-PARP1 interaction, and a p53 activating cytotoxic compound, induces activation of growth arrest and apoptosis signaling in cancer cells in vitro and in vivo.

kt-3283 is a novel bi-functional PARP-HDAC inhibitor with IC50 of 0.338 nM, 2.19 nM and 1.89 uM for PARP1, PARP2 and HDACs, respectively.