Apoptosis

Calcimycin (A-23187) is an antibiotic calcium ionophore that raises intracellular Ca2+ to induce cell death.

AMXT-1501 tetrahydrochloride is an inhibitor of polyamine transport.

Eriosematin has anti-proliferative and apoptosis-inducing properties and is a compound extracted from the root of Flemingia philippinensis in the Philippines.

Bromoiodoacetamide (I-HAcAm): cytotoxic, induces ROS & apoptosis in HepG-2 cells.

CIGB-300 acetate (P15-Tat acetate) is a peptide that acts as an inhibitor of casein kinase 2 (CK2). It exhibits anticancer properties by disrupting the phosphorylation activity of CK2. CIGB-300 acetate induces apoptosis in various tumor cell lines and is applicable for cancer research.

CYP51/PD-L1-IN-4 (compound 14a-2) is a potent dual-target inhibitor of CYP51/PD-L1, displaying IC50 values of 0.17 and 0.021 μM, respectively.

KP1019 is now discontinued.

eIF4A3-IN-7: Potent eIF4A3 inhibitor, potential cancer/dysproliferation research (WO2019161345A1, Compound 8).

<p>eIF4E-IN-3: potent eIF4e inhibitor with promise for cancer study.</p>

RIP2 Kinase Inhibitor 4, a selective RIPK2 PROTAC, degrades RIPK2 (pIC50=8), inhibits TNF-α release.

PI3K/HDAC-IN-4 (Compound 31f) is a dual inhibitor targeting PI3K and HDAC, with an IC50 of 0.2μM. It demonstrates high selectivity for HDAC1-3, with IC50 values of 75.5 nM, 70.9 nM, and 1.9 nM, respectively. As a potent pan-PI3K inhibitor, PI3K/HDAC-IN-4 has IC50 values of 2.5 nM, 80.5 nM, 10.0 nM, and 57.2 nM for PI3Kα, β, δ, and γ, respectively. This compound effectively induces apoptosis in tumor cells by concurrently inhibiting the PI3K/AKT/mTOR signaling pathway and HDAC1-3. It shows significant antiproliferative activity across various tumor cell lines, such as MV4-11, Jeko-1, HL60, and MCF-7, with IC50 values of 0.2, 0.9, 0.8, and 1.5 μM, respectively. PI3K/HDAC-IN-4 is applicable in the study of lymphoma and leukemia.

Theophyllol (theophylline sodium acetate) can alter calcium levels in subcellular fractions of rat brain cortex.

MRIA9 inhibits SIK1/2/3 & PAK2/3 with IC50: SIK1 (516 nM), SIK2 (180 nM), SIK3 (127 nM); ATP-competitive.

JAK/HDAC-IN-2, a potent 2-amino-4-phenylaminopyrimidine dual-target inhibitor, effectively suppresses JAK1/2 and HDAC3/6 at nanomolar concentrations.

BWA-522 is a small molecule, orally available protein-targeting chimera (PROTAC) that potentates the degradation of both full-length androgen receptor (AR-FL)

Estradiol cypionate (Depofemin), the 17 β-cyclopentylpropinate ester of estradiol, inhibits ET-1 synthesis via estrogen receptor.

p53 and MDM2 proteins-interaction-inhibitor dihydrochloride is a interaction inhibitor between p53 and MDM2 proteins.

Anti-inflammatory agent 95 (Compound 2e) is a compound with potent anti-inflammatory properties, showing significant inhibition of NO production in LPS-induced RAW 264.7 mouse macrophages, with an IC50 of 8.8 μM. It also effectively suppresses the secretion of TNF-α and IL-1β, achieving inhibition rates of 60% and greater than 90% at 100 μM, respectively. Anti-inflammatory agent 95 holds promise for research into inflammatory diseases.

icFSP1 is a mitochondria-associated apoptosis-inducing factor regulator with antitumor activity for the study and treatment of tumor diseases.

Arg-Gly-Asp-D-Phe-Val (TFA) has anti-tumor activity and is an inhibitor of integrin αvβ3.