Cyclo(RGDyC) is a cyclic pentapeptide with anti-angiogenic abilities. Cyclo(RGDyC) can be combined with liposome delivery systems for research on ocular neovascular diseases and cancer[1][2].
Salicylic acid-13C6 is the 13C-labeled Salicylic acid (HY-B0167). Salicylic acid is a precursor to and a metabolite of Aspirin (HY-14654), can inhibit cyclo-oxygenase-2 (COX-2) activity[1][2].
N1,N11-Diethylnorspermine (DENSPM) is a potent anticancer agent. N1,N11-Diethylnorspermine is a spermine analog that activates polyamine catabolism. N1,N11-Diethylnorspermine induces the release of cytochrome c from mitochondria, resulting in activation of caspase 3. N1,N11-Diethylnorspermine kills glioblastoma multiforme (GBM) cells through induction of SSAT (spermidine/spermine N1-acetyltransferase) coupled with H2O2 production[1][2][3].
Voreloxin is a first-in-class topoisomerase II inhibitor that intercalates DNA and induces site-selective DNA DSB, G2 arrest, and apoptosis.
N-(Amino-PEG5)-N-bis(PEG4-acid) is a PEG-based PROTAC linker used in the synthesis of PROTACs. N-(Amino-PEG5)-N-bis(PEG4-acid) contains an amino group with two terminal carboxylic acids[1].
USP1-IN-3 is a selective USPI inhibitor. USP1-IN-3 inhibits USPI-UAFI with an IC50 value of ＜30 nM. USP1-IN-3 can be used for the research of cancer[1].
3’-O-Levulinyl-2’-deoxyadenosine 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].
5-Iodouridine 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].
YHO-13351 (free base) is the water-soluble prodrug of YHO-13177, which is a potent and specific inhibitor of BCRP.IC50 value:Target: BCRP inhibitorin vitro: YHO-13177 potentiates the cytotoxicity of SN-38, mitoxantrone, and topotecan in both BCRP-transduced human colon cancer HCT116 (HCT116/BCRP) cells and SN-38-resistant human lung cancer A549 (A549/SN4) cells that express BCRP, but had little effect in the parental cells. In addition, YHO-13177 potentiates the cytotoxicity of SN-38 in human lung cancer NCI-H460 and NCI-H23, myeloma RPMI-8226, and pancreatic cancer AsPC-1 cells that intrinsically expressed BCRP. YHO-13177 increases the intracellular accumulation of Hoechst 33342, a substrate of BCRP, at 30 minutes and partially suppresses the expression of BCRP protein at more than 24 hours after its treatment in both HCT116/BCRP and A549/SN4 cells [1].in vivo: In mice, YHO-13351 is rapidly converted into YHO-13177 after its oral or intravenous administration. Coadministration of irinotecan with YHO-13351 significantly increases the survival time of mice inoculated with BCRP-transduced murine leukemia P388 cells and suppressed the tumor growth in an HCT116/BCRP xenograft model, whereas irinotecan alone has little effect in these tumor models [1].
GNA002 is a potentially and specifically strong EZH2 (Enhancer of zeste homolog 2) inhibitor with an IC50 of 1.1 μM. GNA002 can covalently bind with specific cysteine residue of EZH2 to trigger its ubiquitination and subsequent degradation by the protein quality control E3 ligase, CHIP[1].
3-Epiwilsonine is an alkaloid from Cephalotaxus wilsoniana, exhibits effect on acute and chronic myeloid leukemia and malignant lymphoma[1].
Lorlatinib is a potent, dual ALK/ROS1 inhibitor, with Kis of 0.02 nM, 0.07 nM, and 0.7 nM for ROS1, wild type ALK, and ALK-L1196M, respectively.
Saikosaponin B1 is a component of Saiko, enhances the effect of cancer chemotherapy[1].
m-PEG2-azide is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
E3 Ligase Ligand-Linker Conjugates 19 is a degron-linker. The PROTAC linker is bound lo at least one targeting ligand.
Pasireotide pamoate (SOM230 pamoate) is a stable cyclohexapeptide somatostatin mimic that improves agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9 respectively). Pasireotide pamoate exhibits antisecretory, antiproliferative, and proapoptotic activity[1][2].
c-ABL-IN-3 is a potent inhibitor of c-Abl. Activation of c-Abl has been implicated in various diseases, notably cancer. c-ABL-IN-3 has the potential for the research of neurodegenerative diseases (amyotrophic lateral sclerosis (ALS) and Parkinson’s disease (PD) and cancer (extracted from patent WO2021048567A1, compound 50)[1].
Cobimetinib racemate is the less active racemate of Cobimetinib. Cobimetinib is a potent and selective MEK inhibitor.
Citronellol ((±)-Citronellol) is a monoterpene Pelargonium capitatum. Citronellol ((±)-Citronellol) induces necroptosis of cancer cell via up-regulating TNF-α, RIP1/RIP3 activities, down-regulating caspase-3/caspase-8 activities and increasing ROS (reactive oxygen species) accumulation[1].
Fucoxanthin is a marine carotenoid and shows anti-obesity, anti-diabetic, anti-oxidant, anti-inflammatory and anticancer activities.
SU4984 is a protein tyrosine kinase inhibitor, with an IC50 of 10-20 μM for fibroblast growth factor receptor 1 (FGFR1). SU4984 is also inhibits platelet-derived growth factor receptor, and insulin receptor. SU4984 can be used for the research of cancer[1][2][3].
VL285 Phenol is a VL285 analogue with Phenol group. VL285, a small molecule VHL ligand, can be served as a degrader for HaloPROTAC3 synthesis.VL285 degrades HaloTag7 fusion proteins (IC50=0.34 μM)[1].
Dimethyl-bisphenol A (DMBPA) is a potent HIF-1α inhibitor. Dimethyl-bisphenol A can decrease Vegfa mRNA expression[1].
B-Raf IN 16 (Compound I) is a BRAF inhibitors that belongs a cyclic iminopyrimidine derivative. B-Raf IN 16 can be used for cancer research[1].
20(R)-Ginsenoside Rg2, isolated from Ginseng stems and leaves, shows inhibitory effects on lung cancer NCI-H1650 cells. Anti-cancer activities[1].
RK-33 is an RNA helicase inhibitor against DDX3, and inhibits its helicase activity.
TL4830031 (compound 8i), a quinolone antibiotic derivatives, is a potent Axl inhibitor with an IC50 value of 26 nM. TL4830031 inhibits the phosphorylation of Axl. TL4830031 inhibits cell invasion and migration. TL4830031 can be used for cancer research[1].
EGR240 is a branched-chain amino acid aminotransferase 1 (BCAT1) inhibitor. EGR240 can be used for the research of cancer, rheumatoid arthritis, and bone disease[1].
Antitumor agent-68 is a potent tubulin inhibitor. Antitumor agent-68 shows potent anticancer activity with IC50s of 3.6 and 3.8 µM for HeLa and MCF-7 cells, respectively. Antitumor agent-68 exhibits good scavenging activity of ROS and DPPH radical in a dose-dependent manner[1].
Cyclic di-GMP (c-di-GMP) disodium is a STING activator and a global bacterial second messenger, which regulates biofilm formation, motility, and virulence in diverse bacterial species[1][2].