TL4-12 is a selective MAP4K2/GCK inhibitor, dose-dependently downregulates IKZF1 and BCL-6 and leads to MM cell proliferation inhibition (IC50=37 nM) accompanied by induction of apoptosis. TL4-12 can be used to overcome immunomodulatory drug resistance in multiple myeloma (MM)[1].
MT 63-78 is a specific and potent direct AMPK activator with an EC50 of 25 μM. MT 63–78 also induces cell mitotic arrest and apoptosis. MT 63-78 blocks prostate cancer growth by inhibiting the lipogenesis and mTORC1 pathways. MT 63-78 has antitumor effects[1].
Euscaphic acid, a DNA polymerase inhibitor, is a triterpene from the root of the R. alceaefolius Poir. Euscaphic inhibits calf DNA polymerase α (pol α) and rat DNA polymerase β (pol β) with IC50 values of 61 and 108 μM[1]. Euscaphic acid induces apoptosis[2].
STAT3-IN-11 (7a) is a selective STAT3 inhibitor that inhibits the phosphorylation of STAT3 at site pTyr705. STAT3-IN-11 inhibits the phosphorylation of downstream genes (Survivin and Mcl-1) without affecting its upstream tyrosine kinases (Src and JAK2) levels and p-STAT1 expression. STAT3-IN-11 can induce cancer cell apoptosis, which is potential for the discovery of effective STAT3 inhibitors and antitumor agents against cancers[1].
Laquinimod (ABR-215062) sodium, an orally available carboxamide derivative, is a potent immunomodulator which prevents neurodegeneration and inflammation in the central nervous system. Laquinimod sodium reduces astrocytic NF-κB activation to protect from Cuprizone-induced demyelination. Laquinimod sodium has the potential for relapsing remitting (RR) and chronic progressive (CP) forms of multiple sclerosis (MS; RRMS or CPMS) as well as neurodegenerative diseases research[1][2][3][4].
Temozolomide-d3 (NSC 362856-d3) is the deuterium labeled Temozolomide. Temozolomide (NSC 362856) is an oral active DNA alkylating agent that crosses the blood-brain barrier. Temozolomide is also a proautophagic and proapoptotic agent. Temozolomide is effective against tumor cells that are characterized by low levels of O6-alkylguanine DNA alkyltransferase (OGAT) and a functional mismatch repair system. Temozolomide has antitumor and antiangiogenic effects[1][2].
PI3Kδ-IN-10 is a highly potent and orally active PI3Kδ inhibitor with IC50 of 2 nM. PI3Kδ-IN-10 robustly suppresses the downstream AKT pathway to induce subsequent apoptosis in hepatocellular carcinoma models[1].
9-ING-41 is a potent glycogen synthase kinase-3 (GSK-3) inhibitor[1]. 9-ING-41 induces apoptosis and cell cycle arrest at prophase by targeting centrosomes and microtubule-bound GSK-3β. 9-ING-41 has anticancer activity[2].
BTT-3033 is an orally active conformation-selective inhibitor of α2β1 (EC50: 130 nM) by binding to the α2I domain. BTT-3033 inhibits platelet binding to collagen Ⅰ and cell proliferation, and induces cell apoptosis. BTT-3033 can be used in the research of prostate cancer, inflammation and cardiovascular disease[1][2][4].
A-192621 is a potent, nonpeptide, orally active and selective endothelin B (ETB) receptor antagonist with an IC50 of 4.5 nM and a Ki of 8.8 nM. The selectivity of A-192621 is 636-fold higher than ETA (IC50 of 4280 nM and Ki of 5600 nM). A-192621 promotes apoptosis in PASMCs. A-192621 alos causes elevation of arterial blood pressure and an elevation in the plasma ET-1 level[1][2][3].
Diffractaic acid, a major constituent of U. longissimi, acts as an effective proapoptotic agent in various disorders research[1]. Diffractaic acid is the analgesic and antipyretic component of Usnea diffracta[2].
Citric acid is a weak organic tricarboxylic acid found in citrus fruits. Citric acid is a natural preservative and food tartness enhancer.
Okadaic acid sodium, a marine toxin, is an inhibitor of protein phosphatases (PP). Okadaic acid (sodium) has a significantly higher affinity for PP2A (IC50=0.1-0.3 nM), and inhibits PP1 (IC50=15-50 nM), PP3 (IC50=3.7-4 nM), PP4 (IC50=0.1 nM), PP5 (IC50=3.5 nM), but does not inhibit PP2C. Okadaic acid sodium increases of phosphorylation of a number of proteins by inhibiting PP, and acts a tumor promoter. Okadaic acid sodium induces tau phosphorylation[1][2].
Desacetylcinobufotalin is a natural compound; apoptosis inducer and shows the marked inhibition effect to HepG2 cells and the IC50 value is 0.0279μmol/ml.
cpm-1285 induces apoptosis by functionally blocking intracellular Bcl-2 and related death antagonists. cpm-1285 shows strong binding potency to Bcl-2 with an IC50 value of 130 nM. cpm-1285 reduces tumor burden in mice[1].
Lappaol F, a lignin, is an anticancer agent. Lappaol F inhibits YAP<、b> mRNA and protein level. Lappaol F inhibits tumor cell growth by inducing cell cycle arrest. Lappaol F induces cancer cell apoptosis, and inhibits tumor growth. Lappaol F can be isolated from Arctium lappa Linne (Asteraceae)[1].
S29434 (NMDPEF) is a potent, competitive, selective and cell-permeable inhibitor of quinone reductase 2 (QR2), with IC50s ranging from 5 to 16 nM for human QR2 at different organizational levels, and has good selectivity for QR2 over QR1. S29434 (NMDPEF) induces autophagy and inhibits QR2-mediated ROS production[1].
Ranaconitine is a diterpene alkaloid isolated from A. leucostomum, with cardiotoxicity[1].
3'-Hydroxypterostilbene, a natural pterostilbene analogue, effectively inhibits the growth of human colon cancer cells (IC50s of 9.0, 40.2, and 70.9 µM for COLO 205, HCT-116, and HT-29 cells, respectively) by inducing apoptosis and autophagy. 3'-Hydroxypterostilbene inhibits the PI3K/Akt/mTOR/p70S6K, and p38MAPK pathways and activates the ERK1/2, JNK1/2 MAPK pathways[1].
Anticancer agent 53 is a potent anticancer agent. Anticancer agent 53 shows in vitro cytotoxicity. Anticancer agent 53 induces apoptosis and cell cycle arrest in S/G2/M phases. Anticancer agent 53 shows antitumor activity with no apparent toxicity[1].
Metoprolol fumarate (CGP 2175C) is an orally active, selective β1-adrenoceptor antagonist. Metoprolol fumarate shows anti-inflammation, antitumor and anti-angiogenic properties[1][2][3].
CDK1/2/4-IN-1 (compound 3a) is a potent CDK inhibitor with IC50 values of 1.47, 0.78 and 0.87 μM for CDK1, CDK2 and CDK4, respectively. CDK1/2/4-IN-1 arrests cell cycle at G2/M phase and induces apoptosis. CDK1/2/4-IN-1 elevates Bax, caspase-3, P53 levels and decreases Bcl-2 level. CDK1/2/4-IN-1 can be used for cancer research[1].
Inuviscolide is an apoptosis inducer. Inuviscolide can induce of G2/M arrest in human melanoma cell lines. Inuviscolide exhibits antineoplastic and anti-inflammatory activities[1][2][3].
Mepazine hydrochloride (Pecazine hydrochloride) is a potent and selective MALT1 protease inhibitor with IC50s of 0.83 and 0.42 μM for GSTMALT1 full length and GSTMALT1 325-760, respectively. Mepazine hydrochloride affects viability of ABC-DLBCL cells by enhancing apoptosis[1].
Pheniramine (Prophenpyridamine;Tripoton) is a first-generation histamine H1 receptor antagonist, acts on the central nervous system (CNS) with sedative and hypnotic effect. Pheniramine displays antitumor effect and induces leukemia cells apoptosis. Pheniramine is also a safe and effective local anesthetic, with antipruritic effects[1][2][3][4].
BQZ-485 is a a potent GDI2 inhibitor through the interaction with Tyr245. BQZ-485 disrupts the intrinsic GDI2-Rab1A interaction, thereby abolishing vesicular transport from the endoplasmic reticulum (ER) to the Golgi apparatus and initiating subsequent paraptosis events[1].
Anticancer agent 119 (compound 15) is an N-acylated ciprofloxacin derivative, which has certain antibacterial activity and induces ROS production to promote cancer cell apoptosis[1].
Podocarpusflavone A is a DNA topoisomerase I inhibitor, have moderated anti-proliferative activity induce cell apoptosis in MCF-7, is developing anti-tumor drugstarget: DNA topoisomerase IIn vitro: podocarpusflavone-A show significant inhibitions against DLD, KB, MCF-7, HEp-2 tumor cell lines (ED50 4.56-16.24 μg/mL) and induce cell apoptosis in MCF-7 via mainly sub-G1/S phase arrest. PF (40 ug/mL, 24 hr) significantly induced about 10 folds of cell deaths and growth arrest in S-phase than the control group.
PIK-75 is a reversible DNA-PK and p110α-selective inhibitor, which inhibits DNA-PK, p110α and p110γ with IC50s of 2, 5.8 and 76 nM, respectively. PIK-75 inhibits p110α >200-fold more potently than p110β (IC50=1.3 μM)[1][2]. PIK-75 induces apoptosis[3].
Angophorol is a flavonone compound. Angophorol exerts potential anticancer activity through growth inhibition and apoptosis in K562 cells[1].