DM4-SPDP is a drug-linker conjugate composed of a potent antitubulin agent DM4 and a linker SMCC to make antibody drug conjugate[1]. SPDP is a short-chain crosslinker for amine-to-sulfhydryl conjugation via NHS-ester and pyridyldithiol reactive groups that form cleavable (reducible) disulfide bonds with cysteine sulfhydryls[2][3].
USL311 is a selective CXCR4 antagonist, with anti-tumor activity[1].
LBW242, a 3-mer and Smac mimetic, is a potent and orally active proapoptotic IAP inhibitor. LBW242 shows effects on mutant FLT3-expressing cells. LBW242 has activity against multiple myeloma[1].
BMS-690514 is a potent and orally active inhibitor of EGFR and VEGFR; has IC50s of 5, 20 and 60 nM for EGFR, HER 2 and HER 4, respectively.
CDK4/6/1 Inhibitor is a CDK4/6 inhibitor with IC50s of 3 and 1 nM, respectively.
L-Lysine-d4 is the deuterium labeled L-Lysine. L-lysine is an essential amino acid[1][2][3] with important roles in connective tissues and carnitine synthesis, energy production, growth in children, and maintenance of immu
Gypenoside XLVI is one of the major dammarane-type triterpenoid saponins from Gynostamma pentaphallum[1]. Gypenoside XLVI has a tetracyclic triterpene structure and possess potent non-small cell lung carcinoma A549 cell inhibitory activity[2].
1-Methylpyrene is a fluorescent probe and is also a carcinogen in rodents (λex = 346 nm; λem = 378 nm)[1].
CP21R7 is potent GSK-3β inhibitor, with an IC50 of 1.8 nM; CP21R7 also shows inhibitory activitiy against PKCα, with an IC50 of 1900 nM.
MS143 is a potent AKT degrader (DC50=46 nM and GI50=0.8 µM in PC3 cells). MS143 induces rapid and robust AKT degradation in a concentration- and time-dependent manner via hijacking the ubiquitin-proteasome system. MS143 can suppress cancer cell growth[1].
DM4-SMCC is a drug-linker conjugate for ADC with antitumor activity by using DM4 (an antitubulin agent), linked via the non-cleavable SMCC linker[1].
5-Methyl-2′-O-methyl-uridine (2'-O-methyl-5-methyluridine) 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].
Calcium stearate is a long chain dietary saturated fatty acid which exists in many animal and vegetable fats and oils.
Ingenol 20-palmitate (compound 2) is a diterpene that can be found in Euphorbia lath yris[1].
Lerociclib (G1 T38) dihydrochloride is a potent and selective inhibitor of CDK4/CDK6, with IC50s of 1 nM and 2 nM for CDK4/CyclinD1 and CDK6/CyclinD3, respectively.
Thalidomide-O-amido-C6-NH2 (Cereblon Ligand-Linker Conjugates 11), a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker, can be used in the synthesis of PROTACs[1].
PIK-75 is a DNA-PK and PI3K inhibitor, which inhibits DNA-PK, p110α and p110γ with IC50s of 2, 5.8 and 76 nM, respectively. PIK-75 inhibits p110α >200-fold more potently than p110β (IC50=1.3 μM).
Oleic acid-13C18 (9-cis-Octadecenoic acid-13C18) is the 13C labeled Oleic acid. Oleic acid (9-cis-Octadecenoic acid) is an abundant monounsaturated fatty acid[1]. Oleic acid is a Na+/K+ ATPase activator[2].
Benzyl butyl phthalate-d4 is the deuterium labeled Benzyl butyl phthalate[1]. Benzyl butyl phthalate, a member of phthalic acid esters (PAEs), can trigger the migration and invasion of hemangioma (HA) cells via upregulation of Zeb1. Benzyl butyl phthalate activates aryl hydrocarbon receptor (AhR) in breast cancer cells to stimulate SPHK1/S1P/S1PR3 signaling and enhances formation of metastasis-initiating breast cancer stem cells (BCSCs)[2][3][4].
Itacitinib is a potent and selective inhibitor of JAK1, with >20-fold selectivity for JAK1 over JAK2 and >100-fold over JAK3 and TYK2; Itacitinib is used in the research of myelofibrosis.
αvβ5 integrin-IN-1 is a first potent and selective αvβ5 integrin inhibitor (pIC50 = 8.2) .
Azido-PEG2-CH2COOH is a PEG-based PROTAC linker can be used in the synthesis of PROTACs[1].
3′,5-Dihydroxy-4′,6,7-trimethoxyflavanone is a nature product that could be isolated from the fruits of Vitex rotundifolia. 3′,5-Dihydroxy-4′,6,7-trimethoxyflavanone has potent cytotoxic activity against A549 and HepG-2 cell lines[1].
A non-immunosuppressive FTY720 analogue, PKCδ activator with higher antiproliferative potency with IC50 of 2.4, 2.4, and 3.5 uM in Huh7, Hep3B, and PLC5 cells, respectively; exhibited higher in vitro antiproliferative efficacy relative to FTY720 against HCC cells without cytotoxicity in normal hepatocytes, although devoid of S1P1 receptor activity; induces caspase-dependent apoptosis through ROS-dependent PKCδ activation in HCC tumor cells.
DprE1-IN-2 is a potent DprE1 inhibitor.target: DprE1In vitro: DprE1-IN-2 demonstrats efficacy in a rodent model of tuberculosis, making it promising for further development.
Buspirone is an orally active 5-HT1A receptor agonist. Buspirone is a potent anticancer agent. Buspirone shows antiproliferative activity. Buspirone can be used for anxiety, depression and cancer research[1][2].
NG 52 (Compound 52 ) is a potent, cell-permeable, reversible, selective, and ATP-compatible inhibitor of the cell cycle-regulating kinase, Cdc28p (IC50 = 7 μM), and the related Pho85p kinase (IC50 = 2 μM).IC50 value: 7 uM [1]Target: Cdc28pCompound 52 inhibited growth in a drug-sensitized yeast strainwith a GI 50 of 30 uM. In contrast, the closely related compound 52Me proved to be a significantly weaker inhibitor of yeast growth (GI50=200 uM).
M867 is a selective and reversible inhibitor of caspase-3 with an IC50 of 1.4 nM and Ki of 0.7 nM. M867 has anti apoptotic activity[1].
9-Chloromethyl-10-hydroxy-11-F-Camptothecin is a novel camptothecin derivatives.9-Chloromethyl-10-hydroxy-11-F-Camptothecin is a DNA topoisomerase I (Topo I) inhibitor, can be used in anticancer research[1].
(-)-15-Deoxyspergualin trihydrochloride is a potent antitumor agent. (-)-15-Deoxyspergualin trihydrochloride shows strong inhibition against mouse leukemia L-1210[1].