Venetoclax (GDC-0199; ABT-199) is a highly potent, selective and orally bioavailable Bcl-2 inhibitor with a Ki of less than 0.01 nM.
β-Elemonic acid is a triterpene isolated from Boswellia papyrifera. β-Elemonic acid induces cell apoptosis, reactive oxygen species (ROS) and COX-2 expression and inhibits prolyl endopeptidase. β-Elemonic acid exhibits anticancer and anti-inflammatory effects[1][2].
GEM144 is a potent and orally active DNA polymerase α (POLA1) and HDAC 11 dual inhibitor. GEM144 induces acetylation of p53, activation of p21, G1/S cell cycle arrest, and apoptosis. GEM144 has significant antitumor activity in human orthotopic malignant pleural mesothelioma xenografts[1].
C16-Ceramide is a natural small molecule activating p53 through the direct and selective binding[1].
(6R)-FR054 is an active isomer of FR054. FR054 is an inhibitor of the HBP enzyme PGM3, with a remarkable anti-breast cancer effect. FR054induces endoplasmic reticulum (ER) stress and a ROS-dependent apoptosis[1].
LQZ-7I is a survivin-targeting inhibitor. LQZ-7I inhibits survivin dimerization. LQZ-7I orally effectively inhibits xenograft tumor growth and induces survivin loss in tumors[1].
Anticancer agent 66 (Compound 13e) is an anti-cancer agent. Anticancer agent 66 induces apoptosis and increases sub-G1 cell population in MCF-7 cells. Anticancer agent 66 is a ciprofloxacin analog[1].
Lidocaine hydrochloride hydrate (Lignocaine hydrochloride hydrate) inhibits sodium channels involving complex voltage and using dependence. Lidocaine hydrochloride hydrate decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine hydrochloride hydrate is an amide derivative and has potential for the research of ventricular arrhythmia[1][2].
2,3-DCPE induces apoptosis and downregulates Bcl-XL expression. 2,3-DCPE has anti-tumor activity and can be used in cancer research[1].
δ-Secretase inhibitor 11 (compound 11) is an orally active, potent, BBB-penetrated, non-toxic, selective and specific δ-secretase inhibitor, with an IC50 of 0.7 μM. δ-Secretase inhibitor 11 interacts with both the active site and allosteric site of δ-secretase. δ-Secretase inhibitor 11 attenuates tau and APP (amyloid precursor protein) cleavage. δ-Secretase inhibitor 11 ameliorates synaptic dysfunction and cognitive impairments in tau P301S and 5XFAD transgenic mouse models. δ-Secretase inhibitor 11 can be used for Alzheimer's disease research[1].
Cardanol monoene (Cardanol C15:1) is a phenolic compound which can be found in cashew nut shell liquid. Cardanol monoene can induce mitochondria-associated apoptosis in human melanoma cells[1].
DB1976 hydrochloride is a selenophene analog of DB270 and a potent and cell-permeable fully efficacious transcription factor PU.1 inhibitor. DB1976 hydrochloride potently inhibits PU.1 binding (IC50 of 10 nM) and strongly inhibits the PU.1/DNA complex (with high DB1976-λB affinity, KD of 12 nM) in vitro. DB1976 hydrochloride has apoptosis-inducing effect[1][2][3].
GSK2982772 is a potent and ATP competitive RIP1 inhibitor with an IC50 of 16 nM.
PI3Kδ/γ-IN-3 (Compound 58) is a potent and orally active PI3Kδ and PI3Kγ dual inhibitor with IC50s of 1 nM and 16 nM, respectively. PI3Kδ/γ-IN-3 induces tumor cell apoptosis and can be used for B-cell malignancies research[1].
c-Myc inhibitor 9 (compound 332) is a c-Myc inhibitor with an logEC50 of ≥6. c-Myc inhibitor 9 inhibits tumor growth in nude mouse models. c-Myc inhibitor 9 can be used for cancer research[1].
(+)-Nortrachelogenin (Wikstromol), a pharmacologically ligand from from wikstroemia indica, possesses antileukemic activity[1].
2-Hydroxycinnamaldehyde is a phenylpropanoid that can be isolated from the bark of Cinnamomum cassia. 2-Hydroxycinnamaldehyde inhibits Wnt/β-catenin, STAT3 signaling. 2-Hydroxycinnamaldehyde induces cell apoptosis 2-Hydroxycinnamaldehyde has antitumor and anti-inflammation activities[1][2][3].
PU02, a derivative of 6-MP (HY-13677), is a negative allosteric modulator (NAM) of 5-HT3 receptor, with IC50 values of 0.36 and 0.73 μM in HEK293 cells transfected with human 5-HT3A and 5-HT3AB receptors respectively[1][2].
BCL6 PROTAC 1 is a selective B-cell lymphoma 6 (BCL6) PROTAC. BCL6 PROTAC 1 inhibits BCL6 cell reporter with an IC50 value of 8.8 µM. BCL6 PROTAC 1 significantly degrades BCL6 in diffuse large B-cell lymphoma (DLBCL) cell lines. BCL6 PROTAC 1 can be used in tumor related research[1].
Rilmenidine, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine is an alpha 2-adrenoceptor agonist. Rilmenidine induces autophagy. Rilmenidine modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells[1][2][3].
Terrein is a melanogenesis inhibitor[1]. Terrein induces apoptosis in breast cancer cell lines [2]. Terrein is an inhibitor of quorum sensing and c-di-GMP in Pseudomonas aeruginosa[3].
CPTH2 is a potent histone acetyltransferase (HAT) inhibitor. CPTH2 selectively inhibits the acetylation of histone H3 by Gcn5. CPTH2 induces apoptosis and decreases the invasiveness of a clear cell renal carcinoma (ccRCC) cell line through the inhibition of acetyltransferase p300 (KAT3B)[1][2].
Sanguinarine, a benzophenanthridine alkaloid derived from the root of Sanguinaria Canadensis, can stimulate apoptosis via activating the production of reactive oxygen species (ROS). Sanguinarine-induced apoptosis is associated with the activation of JNK and NF-κB.
EGFR-IN-60 (Compound 7d) shows obvious inhibition of EGFRWT, EGFRT790M, EGFRL858R and JAK3 with IC50s of 83, 26, 53, and 69 nM, respectively. EGFR-IN-60 potently inhibits the growth of H1975 cells harboring EGFRT790M mutation (IC50=1.32 µM) over A431 cells overexpressing EGFRWT (IC50=4.96 µM). EGFR-IN-60 exhibits good oral absorption, potent and safe antitumor activity. EGFR-IN-60 induces cell death through apoptosis supported by increased Bax/Bcl-2 ratio[1].
(R)-CR8 (CR8), a second-generation analog of Roscovitine, is a potent CDK1/2/5/7/9 inhibitor. (R)-CR8 (CR8) inhibits CDK1/cyclin B (IC50=0.09 μM), CDK2/cyclin A (0.072 μM), CDK2/cyclin E (0.041 μM), CDK5/p25 (0.11 μM), CDK7/cyclin H (1.1 μM), CDK9/cyclin T (0.18 μM) and CK1δ/ε (0.4 μM). (R)-CR8 (CR8) induces apoptosis and has neuroprotective effect[1][2].
HSP90-IN-13 (compound 5k) is a highly potent HSP90 pan inhibitor with an IC50 value of 25.07 nM. HSP90-IN-13 has multi-target activity against EGFR, VEGFR-2 and Topoisomerase-2. HSP90-IN-13 causes cell cycle arrest at G2/M phase and induces apoptosis of MCF-7 cells through mitochondrial-mediated pathway[1].
Cedrelone, a limonoid, is a Phenazine biosynthesis-like domain-containing protein (PBLD) activator. Cedrelone induces cancer cell apoptosis, and possess antitumor effects[1].
Oroxin B (OB) is a flavonoid isolated from traditional Chinese herbal medicine Oroxylum indicum (L.) Vent. Oroxin B (OB) possesses obvious inhibitory effect and induces early apoptosis rather than late apoptosis on liver cancer cells through upregulation of PTEN, down regulation of COX-2, VEGF, PI3K, and p-AKT[1].Oroxin B (OB) selectively induces tumor-suppressive ER stress in malignant lymphoma cells[2].
Tripchlorolide is a neuroprotective agent that can be found in Tripterygium wilfordii. Tripchlorolide prevents tumor growth by inducing apoptosis and autophagy. Tripchlorolide improves cognitive deficits in Alzheimer's disease[1][2][3].
Ac-DNLD-CHO (Ac-Asp-Asn-Leu-Asp-CHO) is a Caspase-3/7 inhibitor (IC50: 9.89, 245 nM respectively; Kiapp: 0.68, 55.7 nM respectively). Ac-DNLD-CHO can be used for research of caspase-mediated apoptosis diseases, such as neurodegenerative disorders and viral infection diseases[1].