(S)-(-)-Perillic acid is a terpenoid plant extract with antimicrobial and anticancer activities. (S)-(-)-Perillic acid induces cell apoptosis and cell cycle arrest, and increases the levell of Bax, Bcl2, p21 and caspase-3 proteins. (S)-(-)-Perillic acid can be used for cancer and infection research[1][2][3].
Bleomycin A5 (Pingyangmycin) is an orally active glycopeptide antibiotics. Bleomycin A5 has a role as an antineoplastic agent, an Apoptosis inducer and a bacterial metabolite[1][2].
ML132 (NCGC 00185682) is a potent and selective caspase 1 inhibitor with an IC50 of 0.316 nM.
BMS 310705 (21-Aminoepothilone B) is an analog of Epothilone B (HY-17029), targeting to malignancies such as ovarian, renal, bladder, and lung carcinoma. BMS 310705 induces significant apoptosis via mitochondrial-mediated pathway[1].
Vitexilactone is a diterpenoid that can be isolated from the leaves of Vitex negundo L. Vitexilactone shows antimicrobial activity towards E. coli. Vitexilactone induces cell apoptosis and inhibits cell cycle of cancer cells. Vitexilactone can be used for the research of cancer[1][2].
A novel selective STAT3 inhibitor that inhibits JAK2-STAT3 activation but has no effects on other transcription factors such as NF-κB, and kinases such as AKT, ERK, and c-Src; inhibits STAT3 phosphorylation, dimerization and nuclear translocation, downregulates STAT3-modulated gene expression and induces MM cell apoptosis; delays tumor growth in MM xenograft models (30mg/kg); orally active.
Malic enzyme inhibitor ME1 (ME1) is a multifunctional protein involved in glycolysis, the citric acid cycle, NADPH production, glutamine metabolism, and lipogenesis[1]. Malic enzyme inhibitor ME1 regulates one of the main pathways that provide nicotinamide adenine dinucleotide phosphate (NADPH), which is essential for cancer cell growth through maintenance of redox balance and biosynthesis processes in the cytoplasm. Malic enzyme inhibitor ME1 disrupts metabolism in cancer cells and inhibits cancer cell growth by inducing senescence or apoptosis [2].
[6]-Gingerol is an active compound isolated from Ginger (Zingiber officinale Rosc), exhibits a variety of biological activities including anticancer, anti-inflammation, and anti-oxidation.
Azathioprine (BW 57-322) sodium is an orally active immunosuppressive agent. Azathioprine can be converted in vivo to the active metabolite 6-mercaptopurine (6-MP). Azathioprine has myelosuppressive effects and induces apoptosis[1][3].
CBL0137 hydrochloride is an inhibitor of the histone chaperone, FACT. CBL0137 hydrochloride can also activate p53 and inhibits NF-κB with EC50s of 0.37 and 0.47 µM, respectively.
Polygalacin D (PGD) is a bioactive compound isolated from Platycodon grandiflorum (Jacq.) with anticancer and anti-proliferative properties.PGD suppresses the expression of the IAP family of proteins including survivin, cIAP-1 and cIAP-2 and blocks the PI3K/Akt pathway by inhibiting the phosphorylation of GSK3β, Akt and the expression of PI3K. Polygalacin D induces apoptosis[1]
Antitumor agent-100 (compound A6), an apoptosis inducer and molecular glue, shows superior anti-tumor activity[1].
Anticancer agent 52 is a potent anticancer agent. Anticancer agent 52 shows in vitro cytotoxicity. Anticancer agent 52 induces apoptosis. Anticancer agent 52 shows antitumor effect. Anticancer agent 52 has the potential for the research of bladder cancer[1].
PROTAC eEF2K degrader-1 (Compound 11l) is an eEF2K-Targeting PROTAC small molecule that induces apoptosis in MDA-MB-231 cells. PROTAC eEF2K degrader-1 mediates eEF2K degradation[1].
Citric acid trisodium is a natural preservative and food tartness enhancer. Citric acid trisodium induces apoptosis and cell cycle arrest at G2/M phase and S phase. Citric acid trisodium cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid trisodium causes renal toxicity in mice[1][2][3].
kb NB 142-70 is a potent PKD inhibitor, with IC50s of 28.3, 58.7 and 53.2 nM for PKD1, PKD2, and PKD3, respectively. kb NB 142-70 also has antitumor activity.
PDK4-IN-1 hydrochloride is an anthraquinone derivative and a potent and orally active pyruvate dehydrogenase kinase 4 (PDK4) inhibitor with an IC50 value of 84 nM. PDK4-IN-1 hydrochloride potently represses cellular transformation and cellular proliferation and induces apoptosis. PDK4-IN-1 hydrochloride has antidiabetic, anticancer and anti-allergic activity[1].
1-Alaninechlamydocin, a cyclic tetrapeptide, is a potent HDAC inhibitor (IC50=6.4 nM). 1-Alaninechlamydocin induces G2/M cell cycle arrest and apoptosis in MIA PaCa-2 cells[1].
BO-264 is a highly potent and orally active transforming acidic coiled-coil 3 (TACC3) inhibitor with an IC50 of 188 nM and a Kd of 1.5 nM. BO-264 specifically blocks the function of FGFR3-TACC3 fusion protein. BO-264 induces spindle assembly checkpoint (SAC)-dependent mitotic arrest, DNA damage and apoptosis. BO-264 has broad-spectrum antitumor activity[1].
2-Deoxy-D-glucose-d1 is the deuterium labeled 2-Deoxy-D-glucose. 2-Deoxy-D-glucose is a glucose analog that acts as a competitive inhibitor of glucose metabolism, inhibiting glycolysis via its actions on hexokinase[1][2].
Licoricidin (LCD) is isolated from Glycyrrhiza uralensis Fisch, possesses anti-cancer activities.Licoricidin (LCD) inhibit SW480 cells (IC50=7.2 μM) by inducing cycle arrest, apoptosis and autophagy, and is a potential chemopreventive or chemotherapeutic agent against colorectal cancer[1].Licoricidin (LCD) inhibits Lung Metastasis by inhibition of tumor angiogenesis and lymphangiogenesis as well as changes in the local microenvironment of tumor tissues the anticarcinogenic effect[1].licoricidin enhanced gemcitabine-induced cytotoxicity in Osteosarcoma (OS) cells by inactivation of the Akt and NF-κB pathways in vitro and in vivo[3]. Licoricidin blocks UVA-induced photoaging via ROS scavenging, limits the activity of MMP-1, it can be considered as an active ingredient in new topically applied anti-ageing formulations[4].
Clezutoclax is a potent payload and also a Bcl-XL inhibitor. Clezutoclax can be used in the synthesis of antibody-drug conjugates (ADCs)[1].
Toremifene-d6 (Z-Toremifene-d6) citrate is the deuterium labeled Toremifene citrate. Toremifene citrate (Z-Toremifene citrate) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 µM and 2.6 µM, respectively[1][2].
CCI-007 (CCI 007) is a selective inhibitor of MLL-r, CALM-AF10 and SET-NUP214 leukemia with IC50 of 3.5 uM against MLL-r leukemia cell line PER-485; induced a rapid caspase-dependent apoptosis with mitochondrial depolarization within 24h treatment; altered the characteristic MLL-r gene expression signature in sensitive cells with downregulation of the expression of HOXA9, MEIS1, CMYC and BCL2, important drivers in MLL-r leukemia.
Betulinic acid is a natural pentacyclic triterpenoid, acts as a eukaryotic topoisomerase I inhibitor, with an IC50 of 5 μM, and possesses anti-HIV, anti-malarial, anti-inflammatory and anti-tumor properties.
Thioridazine, an antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs)[1][2][3][4].
GDC-2394 is an orally active and selective NLRP3 inhibitor, and also inhibits IL-1β with IC50s of 0.4 μM (human IL-1β) and 0.1 μM (mouse IL-1β). GDC-2394 inhibits NLRP3-induced caspase-1 activity without inhibiting NLRC4-dependent inflammasome activation[1][2].
dMCL1-2 is a potent and selective degrader of myeloid cell leukemia 1 (MCL1) based on PROTAC, which binds to MCL1 with a KD of 30 nM. dMCL1-2 activats the cellular apoptosis machinery by degradation of MCL1[1].
L-Ascorbic acid-d2 is the deuterium labeled L-Ascorbic acid. L-Ascorbic acid (L-Ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid inhibits selectively Cav3.2 channels with an IC50 of 6.5 μM. L-Ascorbic acid is also a colla