SOP1812 is a naphthalene diimide (ND) derivative with anti-tumor activity. SOP1812 binds to quadruplex arrangements (G4s), and down-regulates several cancer gene pathways. SOP1812 shows great affinity to hTERT G4 and HuTel21 G4 with KD values of 4.9 and 28.4 nM, respectively. SOP1812 can be used for the research of cancer[1].
Anticancer agent 76 (Compound CT2-3) is an anticancer agent. Anticancer agent 76 significantly inhibits the proliferation of human NSCLC cells, induces cell cycle arrest, causes ROS generation and induces cell apoptosis[1].
5’-O-Benzoylthymidine is a thymidine analog. Analogs of this series have insertional activity towards replicated DNA. They can be used to label cells and track DNA synthesis[1].
IQA (CGP-029482) is a potent and selective protein kinase CK2 inhibitor[1].
Macbecin is a stable HSP90 inhibitor by binding to the ATP-binding site with an IC50 of 2 μM and a Kd of 0.24 μM. Macbecin exhibits antitumor and cytocidal activities[1].
Estramustine is an antineoplastic agent. Estramustine depolymerizes microtnbules by binding to tubulin 1, exhibits antimitotic activity with an IC50 value of ~16 μM for mitosis of DU 145 cells. Estramustine blocks cells at mitosis in prostate tumor xenografts[1].
2-Amino-6-meThythio-9-(β-D-ribofuranosyl)-9H-purine 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].
RS-1 is a RAD51 activator, and also increases CRISPR/Cas9-mediated knock-in efficiencies.
5-Hydroxymethyl-2’-β-C-methyluridine 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].
CDK4/6-IN-16 (example 195) is a potent CDK4 and CDK6 inhibitor, with an IC50 of 0.013 μM for CDK4. CDK4/6-IN-16 can be used for the research of CDK4-mediated disorders, such as cancer[1].
hSMG-1 inhibitor 11e is a potent, selective hSMG-1 kinase inhibitor with IC50 of <0.05 nM, >900-fold selectivity over mTOR, and no significant activity against CDK1/2.
2-Amino-7-cyclopropyl methyl-7,8-dihydro-8-oxo-9-(beta-D-xylo furanosyl)purine (G159-82) PTPD-2 Confidential is a purine nucleoside analogue. 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′-O,4′-C-Methyleneguanosine (LNA-G) is a reverse guanine analogue, where LNA (locked nucleic acid) is a nucleic acid analogue. LNA modification can be used in a variety of applications such as effective binding affinity to complementary sequences and greater nuclease resistance than natural nucleotides, offering great potential for applications in disease diagnosis and research. LNA-G is also available via KOD DNA polymerase, which allows the integration of LNA-G nucleotides into the DNA strand[1][2].
GW779439X is a pyrazolopyridazine identified in an inhibitor of the S. aureus PASTA kinase Stk1. GW779439X potentiates the activity of β-lactam antibiotics against various MRSA and MSSA isolates, some even crossing the breakpoint from resistant to sensitive. GW779439X is an AURKA inhibitor and induces apoptosis by the caspases 3/7 pathway[1][2]. MRSA:methicillin-resistant S. aureus; MSSA: methicillin-sensitive S. aureus
Calicheamicin is a cytotoxic agent that causes double-strand DNA breaks.
(2R,3S,5R)-2-(hydroxymethyl)-5-(6-methyl-9H-purin-9-yl)tetrahydrofuran-3-ol (9-(2-Deoxy-beta-D-ribofuranosyl)-6-methylpurine) is a purine nucleoside analogue. 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′,3′-Dideoxy-5-fluorouridine 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].
6-Ethoxy-9-beta-D-(2-C-methyl-ribofuranosyl)purine 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',3',5'-Tri-O-benzoyl-6-azauridine 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].
UPCDC30766 is a potent allosteric inhibitor of p97, with an IC50 of 12 nM. UPCDC30766 can be used for the research of colon cancer[1].
2-Keto-D-galactose (D-Galactosone) inhibits DNA synthesis, and inhibits proliferation of in vitro grown Ehrlich ascites tumor cells[1].
eIF4A3-IN-12 (compound 62) is a silvestrol (HY-13251) analogue. eIF4A3-IN-12 interferes the assembling of eIF4F translation complex with EC50s of 4, 70 and 5 nM for myc-LUC, tub-LUC and the growth inhibition for MBA-MB-231 cells. eIF4A3-IN-12 can be used for the research of human cancer pathogenesis[1].
SIRT1 activator 3 is a potent activator of Sirt1 and suppresses TNF-α in a dose-dependent manner. SIRT1 activator 3 has the potential for anti-obesity or anti-diabetic researches[1].
PARP1-IN-6 is a dual tubulin/PARP-1 inhibitor with IC50 values of 0.94 and 0.48 μM, respectively.
4-Thio-2’-deoxyuridine 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-Chloro-N6-cyclopentyl 2’-deoxy- adenosine 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].
Tinengotinib is the modulator of one or more protein kinases such as Aurora kinase and VEGFR kinase. Tinengotinib has the potential for the research of these kinase abnormalities diseases mediated, especially cancer-related diseases (extracted from patent WO2018108079A1)[1].
POL1-IN-1 is a RNA polymerase 1 (POL1, also known as Pol I) inhibitor with an IC50 of less than 0.5 uM. POL1-IN-1 inhibits ribosome biogenesis by inhibiting POL1 transcription[1].
HDAC6-IN-5 (compound 11b) is a potent and BBB-penetrated HDAC6 inhibitor, with an IC50 of 0.025 μM. HDAC6-IN-5 exhibits strong inhibitory activity against Aβ1-42 self-aggregation and AChE, with IC50 values of 3.0 and 0.72 μM. HDAC6-IN-5 can enhance neurite outgrowth without significant neurotoxicity[1].