Seviteronel (VT-464) R enantiomer is the R enantiomer of Seviteronel (VT-464), which is a potent CYP17 lyase inhibitor(h-Lyase IC50=69 nM); Seviteronel (VT-464) R enantiomer's activity is unknown.
Lucidal (Lucialdehyde C) is a natural lanostante-type triterpene aldehyde that shows inhibitory effects against α-glucosidase (Glucosidase) with an IC50 of 0.635 mM. Lucidal has anticancer and antidiabetic effects[1][2].
Ulenistamab (PBP1510) is a first-in-class hunamised IgG1 monoclonal antibody targeting pancreatic adenocarcinoma upregulated factor (PAUF). Ulenistamab can be used for pancreatic cancer (PC) research[1].
ZMF-10 is a highly potent PAK1 inhibitor, with IC50s of 174 nM, 1.038 μM and 1.372 μM for PAK1, PAK2 and PAK3, respectively. ZMF-10 can inhibit PAK1 activity to affect PAK1-regulated apoptosis, ER-Stress and migration in MDA-MB-231 cells. ZMF-10 can be used for researching anticancer[1].
Anticancer agent 65 (compound 4c) shows excellent activity in cancer cell lines, especially A549 cells, with an IC50 of 1.07 μM. Anticancer agent 65 induces S-phase arrest in A549 cells and increases the expression level of p53 and p21. Anticancer agent 65 causes apoptosis, ROS generation and collapse of MMP in A549 cells[1].
ABT-510 is an anti-angiogenic TSP peptide (Thrombospondin-1 analogue) that induces apoptosis and inhibits ovarian tumour growth in an orthotopic, syngeneic model of epithelial ovarian cancer. ABT-510 also reduces angiogenesis and inflammatory responses in a murine model of inflammatory bowel disease. ABT-510 can be used in studies of cancer (particularly epithelial ovarian cancer) and inflammatory bowel disease (IBD)[1][2].
2-Amino-6-allyl thio-9-(beta-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].
1G244 is a potent DPP8/9 inhibitor with IC50s of 12 nM and 84 nM, respectively. 1G244 does not inhibit DPPIV and DPPII. 1G244 induces apoptosis in multiple myeloma cells and has anti-myeloma effects[1][2].
Folic acid methyl ester is a methyl ester metabolite of folic acid that can be used in the study of neuropsychiatric conditions, such as depression[1].
ZINC00784494 is a specific Lipocalin-2 (LCN2) inhibitor. ZINC00784494 inhibits cell proliferation, cell viability and reduces AKT phosphorylation levels in SUM149 cells. ZINC00784494 has good potential for research in inflammatory breast cancer (IBC)[1].
3',4',5',5,7-Pentamethoxyflavone, a natural flavonoid extracted from Rutaceae plants, sensitizes chemoresistant cancer cells to chemotherapeutic drugs by inhibition of Nrf2 pathway[1].
1-Beta-D-arabinofuranosyl-5-iodouracil 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].
Topoisomerase II inhibitor 3 (Compound 6 h ) is a acridone derivatives, as well as a Type II DNA topoisomerase (topo II) inhibitor , as a topo IIα/β inhibitor with the value of IC50 is 0.17 μM for topo IIα and the value of IC50 is 0.23 μM for topo IIβ subtypes, caused obvious DNA damage, and induced apoptosis by triggering the loss of mitochondrial membrane potential[1].
Triclosan D3 is the deuterium labeled Triclosan. Triclosan is an antibacterial and antifungal agent found in consumer products, including soaps, detergents, toys, and surgical cleaning treatments[1][2].
C-phycocyanin is a water-soluble protein pigment which is also widely used as an excellent nutrient supplement for human beings.
Fumaric acid, associated with fumarase deficiency, is identified as an oncometabolite or an endogenous, cancer causing metabolite.
Aurora inhibitor 1 is a potent Aurora inhibitor with an IC50 of ≤ 4 nM and ≤13 nM for Aurora A and Aurora B kinase, respectively[1].
ATM inhibitor-6 (A-193) is a selective ATM kinase inhibitor. ATM inhibitor-6 can be used in cancer research[1].
MIF-IN-6 (compound 2d) is a potent macrophage migration inhibitory factor (MIF) inhibitor with an IC50 of 1.4 μM and a Ki value of 0.96 μM, respectively. MIF-IN-6 attenuates MIF-induced ERK phosphorylation and inhibits proliferation of A549 cells[1].
AT-533 is a potent Hsp90 and HSV inhibitor. AT-533 suppresses tumor growth and angiogenesis by blocking the HIF-1α/VEGF/VEGFR-2 signaling pathway. AT-533 also inhibits the activation of the downstream pathways, including Akt/mTOR/p70S6K, Erk1/2 and FAK. AT-533 inhibits the tube formation, cell migration, and invasion of human umbilical vein endothelial cells (HUVECs)[1][2][3].
DNA-PK-IN-10 is a DNA-PK inhibitor. DNA-PK-IN-10 can be used for the research of breast cancer and non-small cell lung cancer[1].
Cholesterol myristate is a natural steroid present in traditional Chinese medicine.
ZEN-3862 is a BET inhibitor with IC50s of 0.16 and 0.13 μM for BRD4(BD1) and BRD4(BD2) , respectively. ZEN-3862 can be used to form PROTACs to induce degradation of BRD4[1].
Photosensitizer-2 (compound 1) is a organic D-π-A sensitizer against phototoxicity. Photosensitizer-2 contains an acrylic acid moiety that exerts high levels of phototoxicity. Photosensitizer-2 shows antitumor activity against HeLa cells, with IC50 values of 20.9 ± 4.5 μM (dark) and 0.046 ± 0.012 μM (irradiation), respectively[1].
TK216 directly binds EWS-FLI1 and inhibits EWS-FLI1 protein interactions, leading to a decrease in transcription and proliferation. TK216 blocks the binding between EWS-FLI1 and RNA helicase A. TK216 is active in oncogenesis and inhibits apoptosis[1].
CCG-63802 is a reversible inhibitor of regulator of G-protein signaling (RGS) protein; with greatest potency at RGS4.IC50 value:Target: RGSCCG-63802 is selective amongst RGS proteins, with greatest potency at RGS4. CCG-63802 inhibits GTPase accelerating protein activity of RGS4 and blocks its interaction with Gαo. Retains activity under reducing conditions.
Kaempferol inhibits estrogen receptor α expression in breast cancer cells and induces apoptosis in glioblastoma cells and lung cancer cells by activation of MEK-MAPK.
NOTA is a bifunctional chelate which acts as the framework to construct PET imaging tools. NOTA also can be used for probe design and signal amplification via the multivalent effect[1][2].
JG26 is an ADAM17 inhibitor, with IC50 values of 12 nM, 1.9 nM, 150 nM and 9.4 nM for ADAM8, ADAM17, ADAM10 and MMP-12, respectively[1].
TCRS-417 (T417) is a small molecule compound capable of docking to the interface between PBX1 and its cognate DNA target sequence, effectively interfering with PBX1-DNA interaction. TCRS-417 can be used in the research of cancer, developmental disorders, inflammatory disorders, autoimmune diseases or neurodegenerative diseases[1].