Amantadine (1-Adamantanamine) sulfate is an orally avtive and potent antiviral agent with activity against influenza A viruses. Amantadine sulfate inhibits several ion channels such as NMDA and M2, and also inhibits Coronavirus ion channels. Amantadine sulfate also has anti-orthopoxvirus and anticancer activity. Amantadine sulfate can be used for Parkinson's disease, postoperative cognitive dysfunction (POCD) and COVID-19 research[1][2][3][4][5][6].
BM 957 is a potent Bcl-2 and Bcl-xL inhibitor, with Kis of 1.2, <1 nM and IC50s of 5.4, 6.0 nM respectively.
Ponicidin (Rubescensine B) is a diterpenoid derived from Rabdosia rubescens, and exhibits immunoregulatory, anti-inflammatory, anti-viral and anti-cancer activity. Ponicidin (Rubescensine B) induces apoptosis of gastric carcinoma cell, decreases the phosphorylation of JAK2 and STAT3, and shows no effect on protein levels of JAK2 and STAT3[1].
Forsythoside B is a phenylethanoid glycoside isolated from the leaves of Lamiophlomis rotata Kudo, a Chinese folk medicinal plant for treating inflammatory diseases and promoting blood circulation. Forsythoside B could inhibit TNF-alpha, IL-6, IκB and modulate NF-κB.
Bisdemethoxycurcumin(Curcumin III; Didemethoxycurcumin) is a natural derivative of curcumin with anti-inflammatory and anti-cancer activities.IC50 value:Target: Anticancer natural compoundin vitro: BDMC-induced apoptosis was mediated by a combinatory inhibition of cytoprotective proteins, such as Bcl2 and heme oxygenase-1 and increased generation of reactive oxygen species. Intriguingly, BDMC-induced apoptosis was reversed with co-treatment of sr144528, a cannabinoid receptor (CBR) 2 antagonist, which was confirmed with genetic downregulation of the receptor using siCBR2 [1]. Induction of cell cycle arrest in HepG2 cells by NB and BDCur in combination was evidenced by accumulation of the G2/M cell population. Further investigation on the molecular mechanism showed that NB and BDCur in combination resulted in a significant decrease in the expression level of Cdc2 and cyclin B [2]. BDMC treatment activated Sirt1/AMPK signaling pathway. Moreover, downregulating Sirt1 by the pharmacological inhibitor nicotianamine or small interfering RNA blocked BDMC-mediated protection against t-BHP-mediated decrease in proliferation [4].in vivo: human gastric adenocarcinoma xenograft model was generated in vivo using nude mice and BDMC was observed to suppress the growth and activity of tumors, in addition to improving the physical and mental capacity of the mice [3].
RIPK1-IN-13 (Compound 8) is a potent inhibitor of RIPK1 with an IC50 value of 1139 nM. RIPK1-IN-13 blocks the activation of the necroptosis pathway via the inhibition of RIPK1. RIPK1-IN-13 has the potential for the research of inflammation diseases[1].
Limonin glucoside can be isolated from seeds of Citrus reticulata. Limonin glucoside induces activation of caspase-3. Limonin glucoside inhibits the proliferation of human colon adenocarcinoma (SW480) cells (IC50: 37.39 μM)[1].
6-Hydroxykaempferol 3-O-β-D-glucoside possesses anticancer activity and induces apoptosis[1].
Fisetin is a natural flavonol found in many fruits and vegetables with various benefits, such as antioxidant, anticancer, neuroprotection effects.
Apoptotic agent-2 (compound 14b) induces apoptosis by down-regulation of Bcl-2 and up-regulation of Bax and caspase-3. Apoptotic agent-2 exhibits anti-proliferative activities and can be used for cancer research[1].
FC-11 is a Tubulin inhibitor that effectively inhibits tumor growth in mice. FC-11 can also induce endoplasmic reticulum (ER) stress to generate excess reactive oxygen species (ROS), leading to mitochondrial damage, thereby promoting apoptosis in colorectal cancer (CRC) cells by targeting microtubules. FC-11 can be used in cancer research[1].
Oxybenzone-d5 is the deuterium labeled Oxybenzone[1]. Oxybenzone (Benzophenone 3) is a commonly used UV filter in sun tans and skin protectants. Oxybenzone act as endocrine disrupting chemicals (EDCs) and can pass through the placental and blood-brain barriers. Benzophenone-3 impairs autophagy, alters epigenetic status, and disrupts retinoid X receptor signaling in apoptotic neuronal cells[2][3][4].
PBENZ-DBRMD is a potent iodothyronine deiodinase type 3 (DIO3) inhibitor. PBENZ-DBRMD has anti-proliferative activity and induces apoaptosis. PBENZ-DBRMD can be used for cancer research[1].
Apiole is an anti-tumor agent that induces apoptosis and inhibits human colon cancer cells by inducing G0/G1 cell cycle arrest. Apiole also significantly inhibited colon tumor development in an in vivo mouse xenograft model[1][2].
API-1, a potent Akt/PKB inhibitor, binds to the PH domain and inhibits Akt membrane translocation. API-1 efficiently reduces the phosphorylation levels of Akt with an IC50 of ∼0.8 μM. API-1 is selective for PKB and does not inhibit the activation of PKC, and PKA. API-1 also induces apoptosis by synergizing with TNF-related apoptosis-inducing ligand (TRAIL)[1][2].
N-Methylhemeanthidine chloride is an amaryllidaceae alkaloid isolated from Zephyranthes candida. N-Methylhemeanthidine chloride has antitumor activity and can inhibit cancer cell proliferation by down-regulating < a href=" " class="link-product" target="_blank">AKT activation, mediating cell cycle arrest and inducing < a href=" " class="link-product" target="_blank">apoptosis[1].
Cearoin, isolated from Dalbergia odorifera, increases autophagy and apoptosis through the production of ROS and the activation of ERK[1].
6-Dehydrogingerdione sensitizes human hepatoblastoma hep G2 cells to TRAIL-induced apoptosis via reactive oxygen species-mediated increase of DR5[1].
Amiloride-15N3 (hydrochloride) is the 15N labeled Amiloride hydrochloride[1]. Amiloride hydrochloride (MK-870 hydrochloride) is an inhibitor of both epithelial sodium channel (ENaC[2]) and urokinase-type plasminogen activator receptor (uTPA[3]). Amiloride hydrochloride is a blocker of polycystin-2 (PC2;TRPP2[4]) channel.
Citatuzumab bogatox (VB6-845) is recombinant immunotoxin that composed of Fab fragment of humanized antibody targeting EpCAM and a modified cytotoxin bouganin. Citatuzumab bogatox binds to and selectively induces Apoptosis in EpCAM-positive cell lines and shows good activity in EpCAM-positive human tumour xenograft models[1][2][3].
Illudin S is a sesquiterpene toxin with strong anti-tumour and antiviral activities. Illudin S has genotoxic activities[1][2][3].
LY294002 hydrochloride is a potent and broad-spectrum PI3K inhibitor, with IC50 values of 0.5, 0.57, and 0.97 μM for P110α, P110δ and P110β, respectively. LY294002 hydrochloride also inhibits CK2 with an IC50 of 98 nM. LY294002 hydrochloride can be used for pancreatic cancer research[1][2][3].
Lenalidomide hydrochloride is a potent inhibitor of TNF-α and has antiangiogenic effect. Lenalidomide functions as a protein homeostatic modulator (PHM) linking casein kinase 1A1 (CKIα) to the human E3 ligase cereblon.
Terfenadine-d3 ((±)-Terfenadine-d3) is the deuterium labeled Terfenadine. Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM[1]. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9[2].
ALK-IN-22 (compound I-24) is a potent ALK inhibitor with IC50 values of 2.3, 3.7 and 2.9 nM for ALK, ALKL1196M and ALKG1202R, respectively. ALK-IN-22 down-regulated the phosphorylation of ALK and its downstream proteins. ALK-IN-22 induces apoptosis. ALK-IN-22 can be used for tumor research[1].
Rimiducid (AP1903) is a dimerizer agent that acts by cross-linking the FKBP domains, initiating Fas signaling and hence apoptosis.
PK11007 is a mild thiol alkylator with anticancer activity. PK11007 stabilizes p53 via selective alkylation of two surface-exposed cysteines without compromising its DNA binding activity. PK11007 induces mutant p53 cancer cell death by increasing reactive oxygen species (ROS) levels[1][2].
VAS 3947, a specific NADPH oxidase (NOX) inhibitor, exerts a potent antiplatelet effect. VAS3947 induces apoptosis independently of anti-NOX activity, via UPR activation, mainly due to aggregation and misfolding of proteins[1][2].
Lorlatinib-d3 is the deuterium labeled Lorlatinib. Lorlatinib (PF-06463922) is a selective, orally active, brain-penetrant and ATP-competitive ROS1/ALK inhibitor. Lorlatinib has Kis of <0.025 nM, <0.07 nM, and 0.7 nM for ROS1, wild type ALK, and ALKL1196M
Ac-AAVALLPAVLLALLAP-LEVD-CHO is a cell-permeable caspase-4 inhibitor that has antitumor activity[1].