PT-262 is a potent ROCK inhibitor with an IC50 value of around 5 μM. PT-262 induces the loss of mitochondrial membrane potential and elevates the caspase-3 activation and apoptosis. PT-262 inhibits the ERK and CDC2 phosphorylation via a p53-independent pathway. PT-262 blocks cytoskeleton function and cell migration. PT-262 has anti-cancer activity.

CAY10746 is a selective Rho kinase (ROCK) inhibitor. CAY10746 has inhibitory activity for ROCK I, ROCK II with IC50 values of 0.014 μM and 0.003 μM, respectively. CAY10746 can be used for the research of diabetic retinopathy (DR).

RBN-3143 is a potent and NAD+-competitive catalytic PARP14 inhibitor with an IC50 value of 4 nM. RBN-3143 inhibits PARP14-mediated ADP-ribosylation and stabilizes PARP14 in cell lines. RBN-3143 can be used in research of lung inflammation.

ZIM, a norbornene derived from 4-Aminoantipyrine, is a potent inducer of DNA damage, causing genomic and chromosomal damage as well as inducing cell death and activating phagocytosis. ZIM has chemotherapeutic potential for use in cancer research.

SG2057 (DRG16) is a PBD dimer containing a pentyldioxy linkage which binds sequence selectively in the minor groove of DNA forming DNA interstrand and intrastrand cross-linked adducts. SG2057 is a highly active antitumor agent.

Talotrexin (PT523), an analog of Aminopterin, is a nonpolyglutamatable classic antifolate. Talotrexin is a RFC (reduced folate carrier) specific inhibitor and selectively inhibits RFC transport. Talotrexin shows antitumor activity by targeting DHFR to inhibit tumor growth.

PJ34 is a potent specific inhibitor of PARPl/2 with IC50 of 110 nM and 86 nM, respectively.

Y-27632 2HCl is a selective ROCK1 (p160ROCK) inhibitor with Ki of 140 nM.

WIKI4 is a novel Tankyrase inhibitor with IC50 of 15 nM for TNKS2, and leads to inhibition of Wnt/beta-catenin signaling.

WHI-P180(Janex 3) is a potent inhibitor of IgE-mediated mast cell responses to allergens in vitro and in vivo. Also inhibits cyclin-dependent kinase 2 (CDK2; IC50 = 1µM) by blocking the ATP site

Voreloxin(SNS-595; AG 7352) is a small molecule and a naphthyridine analogue with antineoplastic activity; inhibitor of Topo II.

Volasertib(BI6727) is a highly potent PLK1 inhibitor with an IC50 of 0.87 nM; shows 6- and 65-fold greater selectivity against Plk2 and Plk3.

Veliparib is a potent inhibitor of both PARP-1 and PARP-2 by [3H]NAD+ with Kis of 5.2 and 2.9 nmol/L, respectively.

VE-821 is a potent and selective ATP competitive inhibitor of ATR with Ki and IC50 of 13 nM and 26 nM, respectively.

UPF 1069 is a selective PARP2 inhibitor with IC50 of 0.3 μM; ~27-fold selective against PARP1.

Triapine is a potent ribonucleotide reductase inhibitor with broad spectrum antitumor activity by inhibiting DNA synthesis. Phase 2.

THZ531 is a covalent CDK12 and CDK13 covalent inhibitor.

THZ1 is a novel selective and potent covalent CDK7 inhibitor with IC50(binding affinity) of 3.2 nM; inhibits Jurkat cell's proliferation with IC50 of 50 nM.

Thiazovivin is a rock inhibitor and enhances fibroblast reprogramming efficiency to generate stem cells

TH-302 is selective hypoxia-activated prodrug targeting hypoxic regions of solid tumors with IC50 of 19 nM, demonstrates 270-fold enhanced cytotoxicity under hypoxia versus their potency under aerobic conditions, stable to cytochrome P450 metabolism.

T56-LIMKi is a LIMK2 inhibitor that reduces phosphorylated cofilin, and induces disassembly of actin stress fibers in NF1-/- MEFs cells.

SW-044248 is a Novel Inhibitor of Topoisomerase I Is Selectively Toxic for a Subset of Non-Small Cell Lung Cancer Cell Lines.

SB1317(TG-02) is a novel small molecule potent CDK2/JAK2/FLT3 inhibitor with IC50s of 13/73/56 nM respectively.

SR-3677 is a new potent and selective ROCK-II inhibitor with an IC50 of ~3 nM in enzyme and cell based assays; IC50 for ROCK-I is 56 ± 12 nM.

SNS-032(BMS-387032) is a potent inhibitor of cyclin-dependent kinases (cdks) 9, 2 and 7 (IC50 values are 4, 38 and 62 nM respectively).

SLx-2119(KD-025) is a small molecule and selective inhibitor of ROCK2 with IC50 of 105 nM; > 200 fold selecivity over ROCK1(IC50 =24 uM)

SCH900776 (S-isomer) is the S-isomer form of SCH900776, which is a potent, selective and orally bioavailable inhibitor of checkpoint kinase Chk1 (IC50 = 3 nM), highly selective against Chk2 (IC50 = 1500 nM) and cyclin-dependent kinase CDK2 (IC50

SCH 900776 is a selective Chk1 inhibitor with IC50 of 3 nM. It shows 50-fold selectivity against Chk2. Phase 2.

SAR407899 is a potent, ATP-competitive ROCK inhibitor woth Ki value of 36 nM/41 nM for human ROCK/Rat ROCK respectively.

Ro-3306 is a potent and selective inhibitor of CDK1 with Ki value of 35 nM for CDK1/cyclin B1, 10-fold selectivity relative to CDK2/cyclin E and >50-fold relative to CDK4/cyclin D.