Paederosidic acid is isolated from P. scandens with anticancer and anti‐inflammation activities. Paederosidic acid inhibits lung caner cells via inducing mitochondria-mediated apoptosis[1].
Toddaculin is a natural coumarin that can induce differentiation and apoptosis in leukemic cells. Toddaculin suppresses excess osteoclast activity and enhances osteoblast differentiation and mineralization. Toddaculin also exhibits anti-inflammatory activity[1][2][3].
Evocarpine, a quinolone alkaloid that could be isolated from Evodiae fructus, inhibitss Ca2+ influx through voltage-dependent calcium channels. Antimycobacterial activity[1][2].
AAPK-25 is a potent and selective Aurora/PLK dual inhibitor with anti-tumor activity, which can cause mitotic delay and arrest cells in a prometaphase, reflecting by the biomarker histone H3Ser10 phosphorylation and followed by a surge in apoptosis. AAPK-25 targets Aurora-A, -B, and -C with Kd values ranging from 23-289 nM, as well as PLK-1, -2, and -3 with Kd values ranging from 55-456 nM[1].
Ramipril-d3 is the deuterium labeled Ramipril[1]. Ramipril (HOE-498) is an angiotensin-converting enzyme (ACE) inhibitor with IC50 of 5 nM.
Tebufenozide is a nonsteroidal ecdysone agonist used to control pest. Tebufenozide has cytotoxic and induces apoptosis in HeLa and insect Tn5B1-4 cells[1][2].
Nortriptyline-d3 (Desmethylamitriptyline-d3) hydrochloride is the deuterium labeled Nortriptyline hydrochloride. Nortriptyline hydrochloride (Desmethylamitriptyline hydrochloride) is a tricyclic antidepressant and the main active metabolite of Amitriptyline, and used to relieve the symptoms of depression[1].
CFM-4 is a potent small molecular antagonist of CARP-1/APC-2 binding. CFM-4 prevents CARP-1 binding with APC-2, causes G2M cell cycle arrest, and induces apoptosis with an IC50 range of 10-15 μM. CFM-4 also suppresses growth of drug-resistant human breast cancer cells[1].
BBR-BODIPY is a fluorescent probe that allows screening its interaction with the targeted cells. BBR-BODIPY induces apoptosis and changes the expression of apoptosis-related proteins[1].
PDE5-IN-3 (compound 11j) is a potent PDE5 inhibitor with an IC50 of 1.57 nM. PDE5-IN-3 shows moderate EGFR inhibition with IC50 of 5.827 µM. PDE5-IN-3 significantly inhibits the Wnt/β-catenin pathway (IC50=1286.96 ng/mL). PDE5-IN-3 induces the intrinsic apoptotic mitochondrial pathway in HepG2 cells. PDE5-IN-3 has strong antitumor activity[1].
Apogossypolone (ApoG2) is an orally active Bcl-2 family proteins inhibitor with Ki values of 35, 25 and 660 nM for Bcl-2, Mcl-1 and Bcl-XL, respectively. Apogossypolone shows antitumor activities, induces cell apoptosis[1] and autophagy[2]. Apogossypolone also has antifungal activity[3].
Z-VEID-AFC is a fluorescent substrate for caspase-6[1].
Verminoside is an iridoid isolated from Kigelia africana, exhibits anti-inflammatory and remarkable antioxidant activity with a radical-scavenging activity of 2.5 μg/mL. The genotoxicity of Verminoside on human lymphocytes is associated with elevated levels of PARP-1 and p53 proteins[1][2][3].
c-JUN peptide is a cell-permeable c-JUN-JNK interaction inhibitor. c-JUN peptide inhibits serum-induced c-Jun phosphorylation. c-JUN peptide induces apoptosis[1].
c-Met-IN-10 (compound 26a) is a highly potent c-Met kinase inhibitor with an IC50 value of 16 nM. c-Met-IN-10 has inhibitory activity against cancer cells A549, H460 and HT-29 with IC50s of 0.56 ~ 1.59 μM. c-Met-IN-10 suppresses the colony formation on HT-29 cells, induces HT-29 and A549 cells apoptosis, and inhibits A549 cells motility. c-Met-IN-10 can be used for researching anticancer[1].
Ganoderic acid X is a lanostanoid triterpene that can be extracted from Ganoderma amboinense. Ganoderic acid X inhibits topoisomerases and induces Apoptosis of cancer cells[1].
SF1126 is a clinically relevant pan and dual first-in-class PI3K/BRD4 inhibitor, has antitumor and anti-angiogenic activity. SF1126 is an RGDS-conjugated LY294002 prodrug, which is designed to exhibit increased solubility and bind to specific integrins within the tumor compartment. SF1126 induces cell apoptosis[1].
Justicidin B is a potent anticancer lignan and proapoptotic agent. Justicidin B is also a bone resorption inhibitor, and has strong antiviral, fungicidal, antiprotozoal effects. Justicidin B significantly inhibits platelet aggregation[1][2][3].
Mefuparib hydrochloride is a potent, highly selective, competitive PARP1/2 inhibitor with IC50 of 3.2/1.9 nM, respectively; displays >406-fold over other major nuclear PARPs including PARP3, TNKS1, TNKS2 and PARP6; reduces poly(ADP-ribose) formation, enhances γH2AX levels, induces G2/M arrest and subsequent apoptosis in homologous recombination repair (HR)-deficient cells; shows potent in vitro and in vivo proliferation and growth inhibition against HR-deficient cancer cells and synergistic sensitization of HR-proficient xenografts to the anticancer drug temozolomide.
KT5823, a selective the cGMP-dependent protein kinase (PKG) inhibitor with an Ki value of 0.23 μM, it also inhibits PKA and PKC with Ki values of 10 μM and 4 μM, respectively[1]. KT5823 is a staurosporine-related protein kinase inhibitor, increases thyroid-stimulating hormone-induced (Na+/I- symporter) NIS expression, and iodide uptake in thyroid cells[2]. KT5823 arrests cells after the G0/G1 boundary and causes increases in the levels of apoptotic DNA fragmentation[3].
DCZ3301 is a potent aryl-guanidino inhibitor. DCZ3301 inhibits cell proliferation, induces G2/M cell cycle arrest and apoptosis. DCZ3301 inhibits the activation of the PI3K/AKT pathway by downregulating the protein expression of PI3K and phosphorylation of AKT. DCZ3301 can be used in research of cancer[1].
BAY1082439 is an orally bioavailable, selective PI3Kα/β/δ inhibitor. BAY1082439 also inhibits mutated forms of PIK3CA. BAY1082439 is highly effective in inhibiting Pten-null prostate cancer growth[1][2].
BAI1 is a direct allosteric inhibitor of BAX.
Ginsenoside Rk1 is a unique component created by processing the ginseng plant (mainly Sung Ginseng, SG) at high temperatures[1].Ginsenoside Rk1 has anti-inflammatory effect, suppresses the activation of Jak2/Stat3 signaling pathway and NF-κB[2].Ginsenoside Rk1 has anti-tumor effect, antiplatelet aggregation activities, anti-insulin resistance, nephroprotective effect, antimicrobial effect, cognitive function enhancement, lipid accumulation reduction and prevents osteoporosis[1].Ginsenoside Rk1 induces cell apoptosis by triggering intracellular reactive oxygen species (ROS) generation and blocking PI3K/Akt pathway[3].
Gallic acid-d2 is the deuterium labeled Gallic acid[1]. Gallic acid (3,4,5-Trihydroxybenzoic acid) is a natural polyhydroxyphenolic compound and an free radical scavenger to inhibit cyclooxygenase-2 (COX-2)[2]. Gallic acid has various activities, such as antimicrobial, antioxidant, antimicrobial, anti-inflammatory, and anticance activities[3].
Tamoxifen-d3 is the deuterium labeled Tamoxifen[1]. Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells[2][3][4]. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively[6]. Tamoxifen activates autophagy and induces apoptosis[5]. Tamoxifen also can induce gene knockout of CreER(T2) transgenic mouse[7].
VBIT-3 is an inhibitor of voltage-dependent anion channel 1 (VDAC1) oligomerization with a binding affinity (Kd) of 31.3 μM. VBIT-3, as an apoptosis inhibitor, can be used for therapeutic purposes in apoptosis-associated disorders, such as neurodegenerative and cardiovascular diseases[1].
Cefatrizine (BL-S-640) is an orally active and broad-spectrum cephalosporin antibiotic. Cefatrizine is also a eEF2K inhibitor, with anti-proliferative activity in human breast cancer cells, which could induce ER stress, leading to cell death. Cefatrizine can be used in studies of cancer and bacterial infection[1][2].
PI3K-IN-33 (Compound 6e) is a highly selective PI3K inhibitor with IC50 values of 11.73, 6.09 and 11.18 μM for PI3K-α、PI3K-β and PI3K-δ , respectively. PI3K-IN-33 arrests cell cycle at G2/M phase and induces apoptosis. PI3K-IN-33 can be used in leukemia research[1].