5-Fluorouracil-13C4,15N2 is the 13C and 15N labeled 5-Fluorouracil[1]. 5-Fluorouracil (5-FU) is an analogue of uracil and a potent antitumor agent. 5-Fluorouracil affects pyrimidine synthesis by inhibiting thymidylate synthetase thus depleting intracellular dTTP pools. 5-Fluorouracil induces apoptosis and can be used as a chemical sensitizer[2][3]. 5-Fluorouracil also inhibits HIV[4].
LLP-3 is a potent Survivin inhibitor that disrupts the Survivin-Ran interaction in cancer cells. LLP-3 can be used in the research of Glioblastoma multiforme (GBM)[1].
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.
Asiatic acid, a pentacyclic triterpene found in Centella asiatica, induces apoptosis in melanoma cells. Asiatic acid can be used to treat skin cancer[1]. Asiatic acid also has anti-inflammatory activities[2].
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].
Aeroplysinin 1 ((+)-Aeroplysinin-1), a secondary metabolite isolated from marine sponges, shows potent antibiotic effects on Gram-positive bacteria and exerts antiviral activity against HIV-1 (IC50=14.6 μM). Aeroplysinin 1 has anti-inflammatory, anti-angiogenic and anti-tumor activities. Aeroplysinin 1 induces apoptosis in endothelial cells[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].
LDCA is a dual-hit metabolic modulator and inhibits LDH-A enzyme activity to stimulate apoptosis in the malignant population. LDCA can be used for the research of oncogenic progression[1].
CYD-2-11 is a novel potent, selective Bax agonist that targets the structural pocket proximal to S184 in the C-terminal region of Bax (Ki=34.1 nM); shows no affinity for other Bcl-2 family members; directly activates Bax proapoptotic activity by inducing a conformational change enabling formation of Bax homooligomers in mitochondrial membranes; suppresses malignant growth without evident significant toxicity to normal tissues in mutant KRAS-driven lung cancer models; displays strong synergistic activity and overcomes rapalog resistance combined with RAD001.
Demethylzeylasteral is a triterpene compound isolated from Tripterygium wilfordii Hook F, with anti-inflammatory, immunosuppressive and anti-tumor activities[1][2][3][4][5]. Demethylzeylasteral can significantly alleviates atherosclerosis (AS)[5]. Demethylzeylasteral inhibits triple-negative breast cancer invasion by blocking the canonical and non-canonical TGF-β signaling pathways[2].
Minodronic acid-d4 is deuterium labeled Minodronic acid. Minodronic acid (YM-529) is a third-generation bisphosphonate that directly and indirectly prevents proliferation, induces apoptosis, and inhibits metastasis of various types of cancer cells. Minodronic acid (YM-529) is an antagonist of purinergic P2X2/3 receptors involved in pain[1][2].
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].
C8-Ceramide (N-Octanoyl-D-erythro-sphingosine) is a cell-permeable analog of naturally occurring ceramides. C8-Ceramide has anti-proliferation properties and acts as a potent chemotherapeutic agent. C8-Ceramide stimulates dendritic cells to promote T cell responses upon virus infections. C8-Ceramide induces slight activation of protein kinase (PKC) in vitro[1][2][3][4].
Okadaic acid is extracted from black sponges of the genus Halichondria. Okadaic acid is a non-comepetitive, selective and reversible serine/threonine-specific protein phosphatases 1 (PP1), PP2A and PP3 inhibitor with IC50s of 10-15 nM, 0.5 nM and 4 nM, respectively.[1][2] Okadaic acid eliminate metazoan symbionts/parasites by apoptosis[3].
N,O-Didansyl-L-tyrosine cyclohexylammonium is a potent selective thymidylate synthase (TS) inhibitor，acts on TS of Escherichia coli, Lactobacillus casei and human with the IC50 values of 5.0, 3.4 and 119 μM, respectively[1].
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].
Lapatinib-d4-1 is deuterium labeled Lapatinib. Lapatinib (GW572016) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively[1].
Musk ketone (MK) is a widely used artificial fragrance. Musk ketone shows mutagenic and comutagenic effects in Hep G2 cells and induces neural stem cell proliferation and differentiation in cerebral ischemia via activation of the PI3K/Akt signaling pathway. In the brain, musk ketone is neuroprotective against stroke injury through inhibition of cell apoptosis[1][2][3].
Elesclomol is an oxidative stress inducer that induces cancer cell apoptosis.
Flurbiprofen-13C,d3 is the 13C- and deuterium labeled. Flurbiprofen (dl-Flurbiprofen) is a potent, orally active nonsteroidal anti-inflammatory agent (NSAIA/NSAID), with antipyretic and analgesic activities. Flurbiprofen is commonly used for the research of inflammatory diseases, including osteoarthritis and rheumatoid arthritis. Flurbiprofen is a non-selective cyclooxygenase (COX) inhibitor that can be used for the research of colorectal cancer[1][2][3].
Dihydrorotenone, a natural pesticide, is a potent mitochondrial inhibitor. Dihydrorotenone probably induces Parkinsonian syndrome. Dihydrorotenone induces human plasma cell apoptosis by triggering endoplasmic reticulum stress and activating p38 signaling pathway[1].
Benidipine is a potent and orally active calcium channel antagonist[1]. Benidipine shows anti-apoptosis effects in ischaemic/reperfused myocardial cells[2]. Benidipine increases the activity of endothelial cell-type nitric oxide synthase and improves coronary circulation in hypertensive rats[3].
Ferutinin, a natural terpenoid compound, is an estrogen receptor ERα agonist and estrogen ERβ-receptor agonist/antagonist with IC50s of 33.1 nM and 180.5 nM, respectively. Ferutinin acts as an electrogenic Ca2+-ionophore that increases calcium permeability of lipid bilayer membranes, mitochondria. Ferutinin possesses estrogenic, antitumor, antibacterial and antiinflammatory activities[1][2].
SKI-I is a potent and selective inhibitor of human sphingosine kinase (SK), with an IC50 of 1.2 μM for ST-hSK. SKI-I also inhibits hERK2 (IC50=11 μM). SKI-I induces apoptosis in tumor cell lines[1][2].
Piperazine erastin is an analog of erastin which induces an iron-dependent form of non-apoptotic cell death, termed ferroptosis.
Liensinine Perchlorate is a constituent of Nelumbo nucifera Gaertn, with ani-hypertension and anti-cancer activities. Liensinine Perchlorate induces colorectal cancer (CRC) cell apoptosis[1].
Ac-VAD-pNA is a caspase-1 substrate. Ac-VAD-pNA can be used to detect caspase-1 activity[1].
RIPK1-IN-8 (example 16), an aminoimidazopyridine, is a potent and selective RIPK1 inhibitor with an IC50 of 4 nM. RIPK1-IN-8 has the potential for inflammatory diseases research[1].
Sappanchalcone, a flavonoid isolated from Caesalpinia sappan L., induces caspase-dependent and AIF-dependent apoptosis in human colon cancer cells[1].
Biotin-DEVD-CHO can be used for affinity labeling of Caspase-8 following in vitro caspase cleavage[1].