CDK5-IN-2 (compound 15) is a highly selective CDK5 inhibitor with IC50s of 0.2 and 23 for CDK5/p25 and CDK2/CycA, respectively.

PCLX-001 is an orally acitve, small-molecule, dual N-myristoyltransferase (NMT) inhibitor, with IC50s of 5 nM (NMT1) and 8 nM (NMT2), respectively.

Cdc7-IN-7 (compound I-E) is a potent Cdc7 kinase inhibitor extracted from patent WO2019165473A1, compound I-E. Cdc7 is a serine-threonine protein kinase enzyme which is essential for the initiation of DNA replication in the cell cycle.

Tanuxiciclib trihydrochloride is a cyclin dependent kinase (CDK) inhibitor.

Cdc7-IN-5 (compound I-B) is a potent Cdc7 kinase inhibitor extracted from patent WO2019165473A1, compound I-B. Cdc7 is a serine-threonine protein kinase enzyme which is essential for the initiation of DNA replication in the cell cycle.

Fludarabine triphosphate (F-ara-ATP) trisodium, the active metabolite of Fludarabine, is a potent, noncompetitive and specific inhibitor of DNA primase, with an IC50 of 2.3 μM and a Ki of 6.1 μM. Fludarabine triphosphate trisodium inhibits DNA synthesis by blocking DNA primase and primer RNA formation. Fludarabine triphosphate trisodium inhibits ribonucleotide reductase and DNA polymerase and ultimately leads to cellular apoptosis.

AZ5576 (AZ-5576) is a potent, selective CDK9 inhibitor with an IC 50 <5 nM, decreases phosphorlyation of Ser2-RNAPII in cells with an IC 50 of 96 nM.AZ5576 downregulated Mcl-1 and MYC protein abundance across multiple tested DLBCL cell lines and in primary DLBCL cells.MYC sensitizes DLBCL cells to AZ5576, genetic downregulation of MYC in U-2932 and OCI-LY19 cells resulted in diminished susceptibility to AZ5576.AZ5576 dose-dependently downregulated MYC transcription of a luciferase reporter containing multiple canonical MYC-MAX-binding sites, an effect more pronounced compared with multi-CDK inhibitor dinaciclib.AZ5576 restricts growth of xenografted DLBCL tumors in vivo.

Elomotecan (BN 80927 free base) is a potent inhibitor of topoisomerases I and II. Elomotecan is a camptothecin analog belonging to the homocamptothecin family (hCPT). Elomotecan reduces the proliferation of different tumor cells with higher potency than other anticancer drugs of reference targeting topoisomerases I and II.

MSC-1186 is a highly selective pan-SRPK inhibitor. MSC-1186 has activity for SRPK1, SRPK2 and SRPK3 with IC50 values of 2.7 nM, 81 nM and 0.6 nM, respectively. MSC-1186 can be used for the research of cancer.

WF-536 is an orally active inhibitor of Rho-associated coiled-coil-containing protein kinase (ROCK). WF-536 has tumor anti-metastatic activity. WF-536 can be used for the research of cancer.

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.