DNA Gyrase-IN-3 (Compound 28) is a bacterial DNA gyrase B inhibitor with IC50s of 5.41-15.64 µM for E. coli DNA gyrase. Anti-tubercular and antibacterial activity[1].
Crisnatol (BWA770U) is an orally active and anticancer agent, and a member of the arylmethylaminopropanediol class of DNA intercalators. Crisnatol shows in vitro cytotoxicity against MCF-7 human breast cancer cells, breast cancer cell line (MDA-MB-231), but not normal human skin fibroblasts[1][2][3].
CDK9-IN-10 is a potent CDK9 inhibitor. CDK9-IN-10 is the ligand for the PROTAC CDK9 degrader-2 (HY-112811)[1].
MKC3946 is a potent and soluble IRE1α inhibitor, used for cancer research.
PARP1-IN-7 is an inhibitor of poly(ADP-ribose) polymerase-1 (PARP1) as an anticancer agent.
Tozasertib is the inhibitor of Aurora A/B/C kinases with Kis of 0.6, 18, 4.6 nM, respectively.
Uridine 13C-3 is the 13C labeled Uridine[1].
SB-743921 is a potent inhibitor of the mitotic kinesin KSP (Eg5), with a Ki of 0.1 nM.
4’,5’-Didehydro-2’-O-(2-methoxyethyl)-5-methyluridine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
HDAC8-IN-3 (compound P19) is a potent HDAC8 inhibitor with IC50 value of 9.3 μM and produces thermal stabilization. HDAC8-IN-3 has cytotoxicity and induces apoptosis in leukemic cell lines[1].
2’,3’-Dideoxy-5-fluorocytidine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
2'-C-methyluridine is a uridine analog. Uridine has potential antiepileptic effects, and its analogs can be used to study anticonvulsant and anxiolytic activities, as well as to develop new antihypertensive agents[1].
AMG PERK 44 is an orally active and highly selective PERK inhibitor with an IC50 of 6 nM. AMG PERK 44 has 1000-fold and 160-fold selectivity over GCN2 (IC50=7300 nM) and B-Raf (IC50 >1000 nM), respectively[1][2].
NMS-P715 is a selective, ATP-competitive inhibitor of MPS1, with an IC50 of 182 nM.
3’,5’-Di-O-acetylthymidine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
HEMTAC CDK4/6 degrader 1 is a PROTAC connected by ligands for HSP90 and CDK4/6 with a Kd value of 35.7 μM. HEMTAC CDK4/6 degrader 1 induces CDK4/6 degradation in B16F10 melanoma cells. HEMTAC CDK4/6 degrader 1 arrests cell cycle at G0/G1 phase and induces apoptosis. HEMTAC CDK4/6 degrader 1 can be used in research of cancer[1].
PF 477736 is a potent, selective ATP-competitive inhibitor of Chk1, with a Ki of 0.49 nM, 100-fold selectivity versus Chk2 (Ki, 47 nM).
ε-Amanitin, a cyclic peptide isolated from a variety of mushroom species, potently binds to and inhibits the activity of RNA polymerase II[1][2].
5’-O-(p-Toluoyl)-2’-O-acetyl-3’-deoxy-3’-fluoro-6-chloroinosine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
Vindesine sulfate is a potent tubulin inhibitor with an Ki of 0.110 µM. Vindesine sulfate shows anti-proliferation effect in vitro. Vindesine sulfate shows antitumor effect in vivo[1].
Pirinixic acid (Wy-14643) is a potent agonist of PPARα, with EC50s of 0.63 μM, 32 μM for murine PPARα and PPARγ, and 5.0 μM, 60 μM, 35 μM for human PPARα, PPARγ and PPARδ, respectively.
BAY-1143572 Racemate is the racemate mixture of BAY-1143572. BAY-1143572 is a potent and highly selective, oral P-TEFb/CDK9 inhibitor which supresses CDK9/CycT1 with an IC50 of 13 nM.
THZ531 is a covalent inhibitor of both CDK12 and CDK13 with IC50s of 158 nM and 69 nM, respectively.
Exatecan Intermediate 6 is the intermediate of Exatecan (HY-13631) And Exatecan (DX-8951) is a DNA topoisomerase I inhibitor with an IC50 value of 2.2 μM (0.975 μg/mL) that can be used in cancer research. Exatecan Intermediate 6 can be used to synthesize Antibody-Drug Conjugates (ADCs).
Lometrexol hydrate (DDATHF hydrate), an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol hydrate can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol hydrate has anticancer activity[1][2].
5-Carboxymethylaminomethyluridine is a thymidine analogue. Analogs of this series have insertional activity towards replicated DNA. They can be used to label cells and track DNA synthesis[1].
A2AAR/HDAC-IN-1 (compound 14c) is an orally active, potent and balanced A2AAR/HDAC dual inhibitor, with a Ki of 163.5 nM for A2AAR and an IC50 of 145.3 nM for HDAC1. A2AAR/HDAC-IN-1 shows anticancer activity[1].
Crisnatol (BWA770U) mesylate is an orally active and anticancer agent, and a member of the arylmethylaminopropanediol class of DNA intercalators. Crisnatol mesylate shows in vitro cytotoxicity against human breast cancer cells, but not normal human skin fibroblasts[1][2][3].
Anticancer agent 75 is a potent anticancer agent. Anticancer agent 75 shows cytotoxicity and selectivity in cancer cell lines. Anticancer agent 75 shows cytotoxicity to normal human kidney cell lines is at least 35 times lower than that of the Doxorubicin standard. Anticancer agent 75 shows good activity of antiplasmodial[1].