LEE011 Hcl is an orally available cyclin-dependent kinase (CDK) inhibitor targeting cyclin D1/CDK4 and cyclin D3/CDK6 cell cycle pathway, with potential antineoplastic activity.

ISM042-2-048 is a potent, selective inhibitor of cyclin-dependent kinase 20 (CDK20, cell cycle-related kinase/CCRK) with IC50 of 33.4 nM (CDK20/CycT1), Kd value of 566 nM.

SY-5609 (CDK7-IN-3) is a selective CDK7 inhibitor with a KD of 0.059 nM. CDK7-IN-3 shows poor inhibition on CDK2 (Ki=390 nM), CDK9 (Ki=290 nM), CDK12 (Ki=78 nM). CDK7-IN-3 induce apoptosis in tumor cells and has antitumor activity.

Fraisinib is a specific and effective inhibitor of glycyl-tRNA synthetase 1 (GARS1), suppresses the synthesis of Ap4A by GARS1 and displays strong anti-tumoral potential.

Genz-644282 is a non-camptothecin inhibitor of topoisomerase I with potential antineoplastic activity(IC50=1.2 nM).

RBI2 (Ribosome biogenesis inhibitor 2) is a small molecule inhibitor of ribosome biogenesis inhibitor, potently inhibits pre-rRNA levels in A375 with IC50 of 169 nM.

SYUIQ-5 is a G-quadruplex ligand. SYUIQ-5 stabilizes G-quadruplex and induce senescence. SYUIQ-5 inhibits c-myc gene promoter activity. SYUIQ-5 induces cancer cells autophagy by triggering telomere damage through TRF2 delocalization from telomeres.

Eleutherin ((+)-Eleutherin) is a pyranonaphthoquinones that is isolated from the bulb of Eleutherine americana and a potent catalytic inhibitor of Topoisomerase II. It exhibits potent anti-cancer activity and protects human umbilical vein endothelial cells (HUVECs) from injury in vitro.

ABBV-969 Payload is an agent-linker conjugate with a potent inhibitor of topoisomerase I and a linker designed for use in the antibody-drug conjugate (ADC) ABBV-969. It can be used in non-small cell lung cancer research.

β-Glu-PAB(CH2NH2)-Exatecan (Compound 9a) is a topoisomerase I inhibitor. β-Glu-PAB(CH2NH2)-Exatecan binds to the topoisomerase I-DNA complex to prevent DNA strand reconnection, thereby inducing DNA breakage and cell apoptosis. β-Glu-PAB(CH2NH2)-Exatecan can be specifically cleaved by β-glucuronidase highly expressed in the tumor microenvironment to release Exatecan for cytotoxic effect. β-Glu-PAB(CH2NH2)-Exatecan is also an intermediate of Mal((3S,3aR,6S,6aR) -hexahydrofuro [3, 2-B]furan-3,6-diamine-PEG12)-β -Glu-Pab-Exatecan. β-Glu-PAB(CH2NH2)-Exatecan is promising for research of cancers.

Topotecan acetate is a topoisomerase inhibitor.

OSUAB-0284 is a bacterial topoisomerase inhibitor. OSUAB-0284 has significant anti-staphylococcal activity, especially against methicillin-resistant Staphylococcus aureus (MRSA). OSUAB-0284 exerts its antibacterial effect by inhibiting bacterial topoisomerase. OSUAB-0284 can be used to study infections caused by drug-resistant bacteria such as MRSA.

Mal-Exatecan is a Mal (Maleimide) modified Exatecan. Rilpivirine is an effective and selective diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). It exhibits potent antiviral activity against both wild-type HIV (EC50 = 0.4 nM) and mutant strains (EC50 = 0.1-2.0 nM).

GGFG-PAB-Exatecan TFA consists of an ADC toxin Exatecan-induced allodynia and in PGE2-induced mechanical hyperalgesia. AD353 exhibits a favorable pharmacokinetic profile.

Fostriecin is a triene antibiotic. Fostriecin is a topoisomerase II and protein phosphatase PP2A inhibitor.

AuL1 is an inhibitor of topoisomerase IIα (Top II) with DNA-intercalating properties. AuL1 is cytotoxic to tumor cells and can be used in the research of anticancer agents.

Amrubicin (SM-5887) hydrochloride is a DNA topoisomerase II inhibitor, used for the research of cancer.

8-Chloro-ATP tetrasodium, an ATP analog, is a topoisomerase II (Topo II) inhibitor. 8-Chloro-ATP tetrasodium inhibits DNA synthesis and induces DNA double-stranded breaks (DSBs). 8-Chloro-ATP tetrasodium inhibits Topo II-catalyzed ATP hydrolysis.

8-Chloro-ATP, an ATP analog, is a topoisomerase II (Topo II) inhibitor. 8-Chloro-ATP inhibits DNA synthesis and induces DNA double-stranded breaks (DSBs). 8-Chloro-ATP inhibits Topo II-catalyzed ATP hydrolysis.

(R)-Sitafloxacin (DU-6857), a stereoisomer of Sitafloxacin (DU-6859a), is also an inhibitor of topoisomerases, with an IC50 of 0.18 μg/mL of DNA gyrase.

Ocifisertib hydrochloride (CFI-400945 hydrochloride) is the hydrochloride salt form of Ocifisertib, ONO-AE1-259 (selective EP2 agonist), and acetylcholine. Taprostene sodium exerts a significant cardioprotection.

IIP0943 is a selective inhibitor of PLK1 (polo-like kinase 1), with an IC50 of 5.1 nM for PLK1. In addition, IIP0943 exhibits antiproliferative activity against HCT116 cells, with an IC50 of 0.22 µM. These results suggest that IIP0943 holds promise for research in the field of cancer therapeutics.

ZINC43120769 is a PARP1 inhibitor. ZINC43120769 can be used in prostate cancer (PC) research.

ZINC20906412 is a poly(ADP-ribose) polymerase-10 (PARP10) inhibitor. ZINC20906412 can be used for the research of cancer.

TDI-012804 is a TNKS2 inhibitor that selectively inhibits intracellular endogenous TNKS2 protein. TDI-012804 increases the expression of AXIN1 protein in cells that are heterozygous (Tnks1HET) and completely knocks out (Tnks1KO) for TNKS1. TDI-012804 inhibits the proliferation of ApcQ1405X/Tnks1KO organoids (EC50 of 59.1 nM) and is selectively toxic to Tnks1KO AKP-G12D and AKP-G13D organoids.

KU-0058948 is a specific and potent PARP1 inhibitor with an IC50 of 3.4 nM. KU-0058948 induces cell cycle arrest and apoptosis of primary myeloid leukemic cells and myeloid leukemic cell lines.

Itareparib is the inhibitor for PARP and exhibits antineoplastic activity.

EAPB0503 is a quinoline compound with anti-tumor activity, showing strong cytotoxicity against melanoma cells in vitro (IC50=200 nM). EAPB0503 can induce specific cell cycle arrest in mitosis of CML cells and directly activate apoptosis, leading to an increase in the G0 cell population, disruption of mitochondrial membrane potential, PARP cleavage, and DNA fragmentation. EAPB0503 also reduces the levels of BCR-ABL protein .

BSI-401 is an orally active PARP-1 inhibitor. BSI-401 alone and in synergism with Oxaliplatin. Ocifisertib hydrochloride is an orally active PLK4 inhibitor with a Ki and an IC50 of 0.26 nM and 2.8 nM. Ocifisertib hydrochloride inhibits growth of various cancer cells, arrests cell cycles at G2/M phase, and induces apoptosis. Ocifisertib hydrochloride exhibits antitumor efficacy in mouse model.

Benadrostin is a Poly(ADP-ribose) synthetase inhibitor with an IC50 of 35 μM.