Me-Tet-PEG9-NHS is an ADC Linker containing 9 PEG units. Me-Tet-PEG9-NHS can utilize its own Tetrazine group to undergo a specific inverse electron demand Diels-Alder reaction (iEDDA) with compounds with TCO groups.
Dideoxy-amanitin (compound 2), an α-Amanitin (HY-19610) derivative, is a potent and selective RNA polymerase II allosteric inhibitor with an IC50 value of 74.2 nM[1].
TPI-287, a blood-brain barrier-permeable microtubule stabilizer, can significantly reduce metastatic colonization of breast cancer in the brain[1].
Penpulimab is an IgG1 backbone anti-PD-1 monoclonal antibody with antitumor activities[1].
PI3Kα-IN-9 (compound 27) is a selective, long-acting and oral active PI3Kα inhibitor with IC50 values of 4.4, 128, 146 and 153 nM for PI3Kα, PI3Kγ, PI3Kδ and PI3Kβ, respectively. PI3Kα-IN-9 has antiproliferative activity and induces apoptosis. PI3Kα-IN-9 can be used for cancer research[1].
BT7480 (BCY11863) is one of the Bicycle tumor-targeted immune cell agonists (Bicycle TICAs). BT7480 is an angonist of CD137 (4-1BB). BT7480 consists of a poly(ethylene glycol) (PEG)-based linker, and a synthetic Bicycle peptide targeting CD137 conjugated to Bicycles targeting Nectin-4. Nectin-4 is a cell adhesion molecule, overexpressing in multiple tumor cells. BT7480 elicits significant CD137 agonism and potent antitumor activity in syngeneic mouse models[1][2].
2′-Deoxy-5-nitrocytidine is a DNA Methyltransferase inhibitor extracted from patent CN108498529A. 2′-Deoxy-5-nitrocytidine can be used for the research of cancer[1].
MNK8 is a potent STAT3 (signal transducer and activator of transcription 3) inhibitor. MNK8 inhibits STAT3 activation and reduced its DNA binding ability. MNK8 shows good growth inhibition against hepatocellular carcinoma (HCC) cells. MNK8 induces apoptosis in HCC cells. MNK8 reduces prosurvival proteins expression and migration/invasion of HCC cells[1].
Aminooxy-PEG1-azide is a PEG-based PROTAC linker can be used in the synthesis of PROTACs[1].
Pirenzepine (LS 519 free base) is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine shows anti-proliferative activity to cancer cells[1][2].
Fevipiprant(QAW039) is a selective, potent, reversible competitive CRTh2 antagonist with an in vitro dissociation constant KD value of 1.1nM at the CRTh2 receptor and an IC50 value of 0.44 nM for inhibition of PGD2-induced eosinophil shape change in human whole blood.IC50:0.44 nM(PGD2-induced eosinophil shape change)Kd value:1.1nM(CRTh2 receptor)[1]In vitro: CRTh2-mediated shape change in eosinophils was used to profile QAW039 in whole blood and represents a physiologically relevant environment. The comparable IC50 values for QAW039 in the whole blood and isolated shape-change assays are consistent with its lower plasma-protein binding and its relatively slow dissociation kinetics that drive its increased potency .QAW039 is highly potent in whole-blood systems, with the IC50 value obtained consistent with the affinity values calculated from radioligand experiments. In a further disease-relevant cellular context, the potency of QAW039 in the isolated Th2 cell cytokine inhibition assay is consistent with its CRTh2 receptor affinity, and, as with eosinophil assay readouts, this represents an improved potency compared with QAV680[2].
Figitumumab (CP-751871) is a potent and fully human monoclonal anti–insulin-like growth factor 1 receptor (IGF1R) antibody. Figitumumab prevents IGF1 from binding to IGF1R with an IC50 of 1.8 nM[1].
Xylocytidine is a cytidine analog. Cytidine analogs have a mechanism of inhibiting DNA methyltransferases (such as Zebularine, HY-13420), and have potential anti-metabolic and anti-tumor activities[1].
Nobiletin is a citrus flavonoid with anti-inflammatory, anti-cancer, cholesterol lowering, memory protection activities.
Lecirelin is a synthetic gonadotropin-releasing hormone (GnRH) analogue. Lecirelin is widely used for the research of bovine ovarian follicular cysts[1].
Sinapine is an alkaloid from seeds of the cruciferous species which shows favorable biological activities such as antioxidant and radio-protective activities.
K-Ras-IN-2 (Compound CHI-000-667) is a K-Ras antagonist, and can be used for tumor research[1].
Fmoc-Thr(GalNAc(Ac)3-β-D)-OH inhibits cancer cell growth, through targeting intricate cancer-specific pathways while simultaneously strengthening immunologic response[1].
SB-505124 hydrochloride is a selective inhibitor of TGFβR with IC50 of 129 nM and 47 nM for ALK4, ALK5, respectively, and it does not inhibits ALK1, 2, 3, or 6 but ALK7.
5’(R)-C-Methylguanosine is a guanosine analog. Some guanosine analogs have immunostimulatory activity. In some animal models, they also induce type I interferons, producing antiviral effects. Studies have shown that the functional activity of guanosine analogs is dependent on the activation of Toll-like receptor 7 (TLR7)[1].
Parsaclisib is a potent and selective PI3Kδ inhibitor, with an IC50 of 1 nM at 1 mM ATP, and shows appr 20,000-fold selectivity for PI3Kα, PI3Kβ, PI3Kγ and 57 other kinases.
Heptaplatin (SKI 2053R) is a platinum derivative with anticancer activity against various cancer cell lines, including cisplatin-resistant tumor cell lines. SKI-2053R is active in the research of gastric adenocarcinoma and has favorable toxicity profiles[1].
Pim-1 kinase inhibitor 1 is a Pim-1 kinase inhibitor with an IC50 of 0.11 μM for Pim-1 kinase. Pim-1 kinase inhibitor 1 shows anticancer activity to several cancer cell lines by promotes cell apoptosis. Pim-1 kinase inhibitor 1 can be used for the research of cancer[1].
PD168393 is an potent, cell-permeable, irreversible EGFR inhibitor with IC50 of 0.70 nM, irreversibly alkylate Cys-773, inactive against insulin, PDGFR, FGFR and PKC. target: EGFRIC 50: 0.7 nM [1](1) PD 168393 inhibite EGFr autophosphorylation in A431 human epidermoid carcinoma cells with >9-fold greater potency than PD 174265.[1](2) PD 168393 decrease the production of TNF-α and phosphrylation of ERK1/2 and p38 induced by LPS in cardiomyocytes.[2](3) PD168393 completely inhibits AKT and ERK phosphorylation at concentrations as low as 0.03 umol/L.[3](4) PD168393 could induce apoptosis and inhibit cell growth in ErbB2 positive lung and breast cancer cell lines.[3](5) PD168393 disrupted MEK1/p44/42 ERK signaling in HaCaT cells as determined by inhibition of phospho-p44/42 ERK. [4]
Polatuzumab is a monoclonal antibody, which targets CD79b that is found on the surface of B cells. Polatuzumab sticks to the CD79b protein and delivers the chemotherapy compound into the cell. Polatuzumab can be used to synthesize Polatuzumab Vedotin, which is an antibody-drug conjugate (ADC) targeting CD79b [1].
Crotonoside is isolated from Chinese medicinal herb, Croton. Crotonoside inhibits FLT3 and HDAC3/6, exhibits selective inhibition in acute myeloid leukemia (AML) cells. Crotonoside could be a promising new lead compound for the treatment of AML[1].
Asimicin (Bullatacin) is antitumor acetogenin that can be isolated from the bark and seeds of the pawpaw tree, Asimina trilobal Dunal. Asimicin inhibits mitochondrial respiration through the inhibition of complex I. Asimicin shows toxicity to Aphis gossypii, mosquito larvae and mammalian[1][2][3][4].
ML311 is a potent and selective inhibitor of the Mcl-1/Bim interaction.
m-PEG5-CH2CH2COOH is a PEG-based based PROTAC linker can be used in the synthesis of PROTACs.
BCMA72-80 is a HLA-A2-specific B-cell maturation antigen (BCMA) peptide, with great affinity to HLA-A2, used in the research of multiple myeloma or other B-cell maturation antigen expressing tumors[1].