Delphinidin 3-glucoside chloride (Delphinidin 3-O-glucoside chloride) is an active anthocyanin found in bilberry extract. Delphinidin 3-glucoside chloride induces a pro-apoptotic effect in B cell chronic lymphocytic leukaemia (B CLL)[1]. Delphinidin 3-glucoside chloride exerts phytoestrogen activity by binding to ERβ, with an IC50 of 9.7 μM[2]. Delphinidin-3-O-glucoside chloride inhibits EGFR with an IC50 of 2.37 µM[3].
YM-155 hydrochloride is a novel survivin suppressant with an IC50 of 0.54 nM for the inhibition of survivin promoter activity.
(-)-Hinesol (Hinesol) is a potent anticancer agent. (-)-Hinesol induces apoptosis and cell cycle arrest at G0/G1 phase. (-)-Hinesol downregulates MEK/ERK pathway and NF-κB pathway and mediates theexpression of cyclin D1, Bax and Bcl-2. (-)-Hinesol has the potential for the research of non–small cell lung cancer[1].
15-acetoxyscirpenol, one of acetoxyscirpenol moiety mycotoxins (ASMs), strongly induces apoptosis and inhibits Jurkat T cell growth in a dose-dependent manner by activating other caspases independent of caspase-3[1].
Bisindolylmaleimide VIII acetate (Ro 31-7549 acetate) is a potent and selective protein kinase C (PKC) inhibitor with an IC50 of 158 nM for rat brain PKC. Bisindolylmaleimide VIII acetate has IC50s of 53, 195, 163, 213, and 175 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, PKC-ε, respectively[1]. Bisindolylmaleimide VIII acetate facilitates Fas-mediated apoptosis and inhibits T cell-mediated autoimmune diseases[2].
Tubulin polymerization-IN-22 is a tubulin polymerization inhibitor with an IC50 of 8.1 μM. Tubulin polymerization-IN-22 arrests cell cycle at G2/M phase and induces apoptosis[1].
MRT 199665 is a potent salt-inducible kinases (SIKs) inhibitor with IC50 of 110, 12, 43 nM for SIK1,2,3 respectively; also inhibits AMPKα1/α2 (both IC50=10 nM), MARK1/2/3/4 (both IC50=2 nM), NUAK1/2 (IC50=3/120 nM), and MELK (IC50=29 nM); elevates IL-10 production by inducing the dephosphorylation of CREB-regulated transcriptional coactivator 3 (CRTC3), increases LPS-stimulated IL-10 production and greatly suppressed proinflammatory cytokine secretion (IL-6, IL-12, and TNF) in macrophages.
Citreoviridin, a toxin from Penicillium citreoviride NRRL 2579, inhibits brain synaptosomal Na+/K+-ATPase whereas in microsomes, both Na+/K+-ATPase and Mg2+-ATPase activities are significantly stimulated in a dose-dependent manner[1]. Citreoviridin inhibits cell proliferation and enhances apoptosis of human umbilical vein endothelial cells[2].
Clitocine, an adenosine nucleoside analog, is a potent and efficacious readthrough agent. Clitocine can induce the production of p53 protein in cells harboring p53 nonsense-mutated alleles. Clitocine can induce apoptosis in multidrug-resistant human cancer cells by targeting Mcl-1. Anticancer activity[1][2].
RIPA-56 is a highly potent, selective, and metabolically stable inhibitor of receptor-interacting protein 1 (RIP1) with an IC50 of 13 nM.
GSK2593074A (GSK’074) is a necroptosis inhibitor with dual targeting ability to both RIP1 and RIP3[1].
WDR5-IN-1 is a potent and selective WD repeat domain 5 (WDR5) inhibitor, with a Kd of <0.02 nM. WDR5-IN-1 inhibits MLL1 histone methyltransferase (HMT) activity with an IC50 of 2.2 nM. WDR5-IN-1 diminishes MYC recruitment at WDR5-displaced genes and exhibits potent anti-proliferative effects in CHP-134 (neuroblastoma) and Ramos (Burkitt’s lymphoma) lines[1].
Lacto-N-fucopentaose I (LNFPI) is a human milk oligosaccharide (HMO), possessing antiviral and antibacterial activity. Lacto-N-fucopentaose I can reduce capsid protein VP1 to block virus adsorption, promote CDK2 and reduce cyclin E to recover cell cycle S phase block. Lacto-N-fucopentaose I inhibits ROS production and apoptosis in virus-infected cells. Lacto-N-fucopentaose I can also regulate intestinal microbiota to affect immune system development[1].
Jolkinolide A is a diterpenoid, can be extracted from the roots of Euphorbia fischeriana Steud. Jolkinolide A exhibits anti-tumor activity, by affecting on angiogenesis of tumor tissues. Jolkinolide A significantly inhibits the Akt-STAT3-mTOR signaling pathway and reduces the expression of VEGF in A549 cells[1].
BM-1244 is a potent Bcl-xL/Bcl-2 inhibitor with Kis of 134 and 450 nM for Bcl- xL and Bcl-2, respectively. BM-1244 inhibits senescent fibroblasts (SnCs) with an EC50 of 5 nM. (From patent WO2019033119A1)[1].
Glyphosate-d2 is the deuterium labeled Glyphosate. Glyphosate is an herbicidal derivative of the amino acid glycine. Glyphosate targets and blocks a plant metabolic pathway not found in animals, the shikimate pathway, required for the synthesis of aromatic amino acids in plants[1].
Mepazine (Pecazine) is a potent and selective MALT1 inhibitor. Mepazine inhibits GSTMALT1 full length and GSTMALT1 325-760 with IC50s of 0.83 and 0.42 μM, respectively. Mepazine affects viability of ABC-DLBCL cells by enhancing apoptosis[1].
Lusianthridin, a pure compound from Dendrobium venustum, have an anti-migratory effect. Lusianthridin enhances c-Myc degradation through the inhibition of Src-STAT3 signaling[1].
KTX-582 is a potent IRAK4 degrader with DC50 values of 4 nM and 5 nM for IRAK4 and Ikaros, respectively. KTX-582 can induce apoptosis in MYD88MT DLBCL, and is efficient to induce in vivo tumor regressions in lymphoma model[1][2][3].
ZDLD13, a β-carboline, is an orally active and selective CDK4/CycD3 inhibitor with an IC50 value of 0.38 μM. ZDLD13 exhibits potent anti-HCT116 activity including inhibition of colony formation, inhibition of invasion and migration, inducing of apoptosis, and arresting of G1 phase in cell cycle. ZDLD13 shows significant tumor growth inhibition in HCT116 tumor xenograft model[1].
Tubulin inhibitor 33, a tubulin polymerization inhibitor, inhibits tubulin polymerization in a dose-dependent manner with an IC50 of 9.05 μM. Tubulin inhibitor 33 has antitumor effects and induces cell apoptosis that can be used for antitumor research[1].
Mcl1-IN-12 (Compound F) is a selective Mcl-1 inhibitor, less potent at Bcl-2, with Kis of 0.29 and 3.1 μM, respectively. Anti-tumor activity[1].
β-Naphthoflavone is a non-carcinogenic AhR agonist as a positive control for the induction of AhR transcriptional activity[1]. β-Naphthoflavone inhibits hydrogen peroxide-induced apoptosis[2].
Amsilarotene (TAC-101; Am 555S), an orally active synthetic retinoid, has selective affinity for retinoic acid receptor α (RAR-α) binding with Ki of 2.4, 400 nM for RAR-α and RAR-β. Amsilarotene induces the apoptotic of human gastric cancer, hepatocellular carcinoma and ovarian carcinoma cells. Amsilarotene can be used for the research of cancer[1][2][3].
8-prenylnaringenin is a prenylflavonoid isolated from hop cones (Humulus lupulus), with cytotoxicity. 8-prenylnaringenin has anti-proliferative activity against HCT-116 colon cancer cells via induction of intrinsic and extrinsic pathway-mediated apoptosis. 8-Prenylnaringenin also promotes recovery from immobilization-induced disuse muscle atrophy through activation of the Akt phosphorylation pathway in mice[1] [2] [3].
CM-272 (CM272) is a novel potent, selective and reversible dual inhibitor of G9a/DNMTs with IC50 of 8 nM and 382 nM for G9a and DNMT1, respectively; also inhibits DNMT3A/3B/GLP with IC50 of 85/1,200/2 nM, respectively; inhibits cell proliferation and promotes apoptosis in different haematological neoplasias (AML, ALL and DLBCL); significantly prolongs survival of AML, ALL and DLBCL xenogeneic models.
Higenamine (Norcoclaurine), a β2-AR agonist, is a key component of the Chinese herb aconite root that prescribes for treating symptoms of heart failure in the oriental Asian countries. Higenamine (Norcoclaurine) has anti-apoptotic effects[1][2].
Topoisomerase II inhibitor 10 (compound 32a) is a potent topoisomerase II inhibitor with an IC50 value of 7.45 μM. Topoisomerase II inhibitor 10 causes cell cycle arrest at G2-M phase and induces apoptosis of HepG-2 cells. Topoisomerase II inhibitor 10 has excellent anti-proliferative activities against HepG-2, MCF-7, and HCT-116 cells[1].
Perillic acid is the metabolite of Perillyl alcohol (HY-N7000). Perillic acid induces lung cancer cell cycle arrest and apoptosis. Perillic acid shows anti-HSV-1 and immunomodulatory activities[1][2][3].
Ungeremine, a phenanthridine type alkaloid, is extracted of the bulbs of Pancratium Illyricum. Ungeremine effectively targets mammalian as well as bacterial type I and type II topoisomerases. Ungeremine displays cytotoxic activity towards the 9 cancer cell lines, including drug-sensitive and MDR phenotypes. Ungeremine induced ferroptosis, necroptosis, autophagy as well as apoptosis mediated by caspase activation, MMP alteration and increase ROS production[1][2].