ZX-29 is a potent and selective ALK inhibitor with an IC50 of 2.1 nM, 1.3 nM and 3.9 nM for ALK, ALK L1196M and ALK G1202R mutations, respectively. ZX-29 is inactive against EGFR. ZX-29 induces apoptosis by inducing endoplasmic reticulum (ER) stress and overcomes cell resistance caused by an ALK mutation. ZX-29 also induces protective autophagy and has antitumor effect[1].
Bonannione A (6-Geranylnaringenin; Mimulone), a prenylflavonoid, is an orally active and potent protein tyrosine phosphatase 1B (PTP1B) inhibitor with an IC50 of 14 µM. Bonannione A triggers caspase-dependent Apoptosis. Bonannione A induces Autophagy through p53-mediated AMPK/mTOR pathway. Bonannione A shows anti-inflammatory, antiradical and anti-cancer activity[1][2][3].
DMUP is a potent CD47-SIRPα axis inhibitor. DMUP induces apoptosis and increases the macrophage phagocytosis in A549 cells. DMUP decreases the expression of CD47 and SIRPα protein. DMUP shows antitumor activity[1].
MitoTam iodide, hydriodide is a tamoxifen derivative[1], an electron transport chain (ETC) inhibitor, spreduces mitochondrial membrane potential in senescent cells and affects mitochondrial morphology[2].MitoTam iodide, hydriodide is an effective anticancer agent, suppresses respiratory complexes (CI-respiration) and disrupts respiratory supercomplexes (SCs) formation in breast cancer cells[1][2]. MitoTam iodide, hydriodide causes apoptosis[2].
Simvastatin acid (Tenivastatin) is an orally active HMG-CoA reductase (HMGCR) inhibitor. Simvastatin acid can reduce cholesterol synthesis and lower blood cholesterol levels[1]. Simvastatin acid shows anti-proliferation activities against cancer cells and induces apoptosis[2].
L-Glutamic acid-13C2 is the 13C labeled L-Glutamic acid[1]. L-Glutamic acid acts as an excitatory transmitter and an agonist at all subtypes of glutamate receptors (metabotropic, kainate, NMDA, and AMPA). L-Glutamic acid shows a direct activating effect on the release of DA from dopaminergic terminals[2].
2-Deoxy-D-glucose-13C is the 13C 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].
Lupalbigenin is a natural compound with anti-metastatic and pro-apoptotic effects[1].
Cabozantinib-d4 is deuterium labeled Cabozantinib. Cabozantinib is a potent multiple receptor tyrosine kinases (RTKs) inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.
Pinosylvin is a pre-infectious stilbenoid toxin isolated from the heartwood of Pinus spp, has anti-bacterial activities[1]. Pinosylvin is a resveratrol analogue, can induce cell apoptosis and autophapy in leukemia cells[2].
NEDD8 inhibitor M22 is a novel, potent, selective reversible NEDD8 activating enzyme (NAE) inhibitor; inhibit A549 cell proliferation completely at 30 uM (GI50=5.5 uM and GI90=19.3 uM); produces tumor inhibition in AGS xenografts in nude mice and low acute toxicity in zebrafish model; exhibts different binding mode compared with MLN4924.
Ketoprofen-13C,d3 is the 13C- and deuterium labeled. Ketoprofen (RP-19583) is a non-steroidal antiinflammatory agent, acting as a potent inhibitor of COX, with IC50s of 2 nM and 26 nM for COX-1 and COX-2 in human blood monocytes, respectively[1].
AT9283 lactic acid is a multi-targeted kinase inhibitor with potent activity against Aurora A/B, JAK2/3, Abl (T315I) and Flt3 (IC50s ranging from 1 to 30 nM). AT9283 lactic acid inhibits growth and survival of multiple solid tumors in vitro and in vivo[1][2].
PTC-028 is an orally bioavailable inhibitor of stem cell factor BMI-1 in ovarian cancer. PTC-028 selectively inhibits cancer cells whereas normal cells remain unaffected. Depletion of BMI-1 by PTC-028 induces caspase-mediated apoptosis[1].
Dauricine, a bisbenzylisoquinoline alkaloid in Asiatic Moonseed Rhizome, possesses anti-inflammatory activity. Dauricine inhibits cell proliferation and invasion, and induces apoptosis by suppressing NF-κB activation in a dose- and time-dependent manner in colon cancer[1].
XMU-MP-3 is a potent non-covalent BTK inhibitor with IC50s of 10.7 nM and 17.0 nM for BTK WT and BTK C481S mutation in the presence of 10 μM ATP, respectively. XMU-MP-3 also induces apoptosis[1].
Polyporenic acid C is a lanostane-type triterpenoid isolated from P. cocos. Polyporenic acid C induces cell apoptosis through the death receptor-mediated apoptotic pathway without the involvement of the mitochondria. Polyporenic acid C is promising agent for lung cancer therapy[1].
A non-immunosuppressive FTY720 analogue, PKCδ activator with higher antiproliferative potency with IC50 of 2.4, 2.4, and 3.5 uM in Huh7, Hep3B, and PLC5 cells, respectively; exhibited higher in vitro antiproliferative efficacy relative to FTY720 against HCC cells without cytotoxicity in normal hepatocytes, although devoid of S1P1 receptor activity; induces caspase-dependent apoptosis through ROS-dependent PKCδ activation in HCC tumor cells.
Moroidin (1) is a bicyclic octapeptide belonging to the Urticaceae-type cyclopeptide family. Moroidin (1) has a potent inhibitory effect on purified tubulin polymerization. Moroidin (1) has cytotoxic effects for several cancer cells, and can induce apoptosis in A549 human lung cancer cells[1].
8-Aminoadenosine (8-NH2-Ado), a RNA-directed nucleoside analogue, reduces cellular ATP levels and inhibits mRNA synthesis. 8-Aminoadenosine blocks Akt/mTOR signaling and induces autophagy and apoptosis in a p53-independent manner. 8-Aminoadenosine has antitumor activity[1][2][3].
Lacidipine-d10 is the deuterium labeled Lacidipine. Lacidipine (Lacipil, Motens) is a L-type calcium channel blocker[1][2].
RA-9 is a potent and selective proteasome-associated deubiquitinating enzymes (DUBs) inhibitor with favorable toxicity profile and anticancer activity. RA-9 blocks ubiquitin-dependent protein degradation without impacting 20S proteasome proteolytic activity. RA-9 selectively induces onset of apoptosis in ovarian cancer cell lines and primary cultures derived from donors. RA-9 induces endoplasmic reticulum (ER)-stress responses in ovarian cancer cells[1].
Illudin M is a cytotoxic fungal sesquiterpene that can be isolated from the culture medium of Omphalotus olearius mushrooms. Illudin M can alkylate DNA. Illudin M has anti-tumor activities[1][2].
Kp7-6, a Fas mimetic peptide, is a Fas/FasL antagonist. Kp7-6 protects cells from Fas-mediated apoptosis, and protects mice from Fas-mediated hepatic injury[1][2].
NSC697923 is a potent UBE2N (ubiquitin-conjugating enzyme E2 N, Ubc13) inhibitor. NSC697923 induces neuroblastoma (NB) cell death via promoting nuclear importation of p53 in p53 wild-type NB cells. NSC697923 also induces cell death in p53 mutant NB cells by activation of JNK-mediated apoptotic pathway. NSC697923 inhibits DNA damage and NF-κB signaling. Antitumor activity[1][2].
CSRM617 hydrochloride (CSRM-617) is a small-molecule inhibitor of the transcription factor ONECUT2 (OC2) with Kd of 7.43 uM in SPR assays, binds to OC2-HOX domain directly; inhibits cell growth and induced apoptosis in vitro in several PC cell lines that expressed moderate to high levels of OC2; significantly downregulates PEG10 protein levels in tumors from mice treated with CSRM617, suppresseses metastasis in 22Rv1 cells implanted subcutaneously nude mice.
Soyasapogenol B, an ingredient of soybean, exerts anti-proliferative, anti-metastatic activities. Soyasapogenol B triggers endoplasmic reticulum stress, which mediates apoptosis and autophagy in colorectal cancer[1][2].
Phytosphingosine is a phospholipid and has anti-cancer activities. Phytosphingosine induces cell apoptosis via caspase 8 activation and Bax translocation in cancer cells[1].
Ono 3403 is a synthetic serine protease inhibitor. Ono 3403 inhibits lipopolysaccharide-induced tumor necrosis factor-alpha and nitric oxide production. ONO-3403 also has an antitumor effect on malignant tumors.
DC-U4106 is a USP8 targeting inhibitor with the Kdvalue of 4.7 μM and the IC50 value of 1.2 μM. DC-U4106 can target the ubiquitin pathway and facilitate the degradation of Erα. DC-U4106 inhibits tumor growth with minimal toxicity and has the potential for the research of breast cancer[1].