Caspase Modulator

Fezakinumab (ILV 094) is an anti-IL-22 monoclonal antibody. Fezakinumab inhibits IL-22 signal transduction, and regulates the JAK1/STAT3 pathway as well as apoptotic proteins. Fezakinumab alleviates airway remodeling, alveolar enlargement and inflammatory cell infiltration in lung tissues. Fezakinumab reduces the levels of neutrophils, lymphocytes, eosinophils and macrophages in lung tissues. Fezakinumab can be used in the research of chronic obstructive pulmonary disease and skin diseases.

Lacidipine is an orally active and highly selective L-type calcium channel blocker that acts on smooth muscle calcium channels, primarily dilates peripheral arteries, reduces peripheral resistance, and has long-lasting anti-hypertensive activity. Lacidipine protects HKCs from apoptosis induced by ATP depletion and recovery by modulating the caspase-3 pathway. Lacidipine can be used in studies of hypertension, atherosclerosis and acute kidney injury (AKI).

Rehmannioside D is an orally active Sirt7 modulator. Rehmannioside D upregulates Sirt7 expression, inhibits the level of acetylated p53, and blocks the activation of the p53 signaling pathway. Rehmannioside D alleviates liver injury, inflammatory response, collagen deposition and hepatocyte apoptosis. Rehmannioside D is applicable to research related to liver fibrosis.

HDAC9-IN-1 is a selective class IIa HDAC inhibitor that binds to HDAC9 with an IC₅₀ of 40 nM. HDAC9-IN-1 potently inhibits HDACs 4 and 7 while showing weak activity against HDAC6 (IC₅₀ values: 180 nM (HDAC4), 190 nM (HDAC7), 970 nM (HDAC6)). HDAC9-IN-1 significantly inhibits several human cancer cells, induces apoptosis and DNA damage in human cancer cells, and modulates caspase-related proteins and p38 in human cancer cells. HDAC9-IN-1 can be used for the research of oral cancer, breast cancer, gastric cancer.

RSM3 is a METTL3-METTL14 complex inhibitor with a K_d of 3.10 μM for the METTL3-METTL14 complex. RSM3 reduces the m⁶A modification level of SLC31A1 and the global RNA methylation level. RSM3 upregulates programmed cell death-related genes, enhances cell apoptosis, inhibits pro-cancer signals and suppresses tumor growth. RSM3 is applicable to the research of preeclampsia and cancer.

Macranthoidin B (Macranthoiside I) is an orally active triterpene saponin. Macranthoidin B inhibits epithelial-mesenchymal transition in endometriosis via the COX‑2/PGE2 pathway, and also induces tumor cell apoptosis and inhibits their proliferation by regulating metabolism and increasing ROS levels. Macranthoidin B can be used in studies related to endometriosis, colorectal cancer and hepatocellular carcinoma.

SKLB-Y13 is a selective YTHDF1 inhibitor with an IC₅₀ of 0.76 μM and a K_D of 5.097 μM. SKLB-Y13 binds to the Tyr397 and Trp470 residues in the m⁶A-binding pocket of YTHDF1, disrupting the interaction between YTHDF1 and m⁶A-modified mRNA. SKLB-Y13 inhibits cancer cell proliferation and promotes apoptosis. SKLB-Y13 is applicable to breast cancer-related research.

ASTX295 is an orally active and selective MDM2 antagonist with an IC₅₀ of <1 nM. ASTX295 inhibits the MDM2-p53 interaction, activates wild-type TP53, and thereby induces the expression of relevant transcriptional targets, leading to cell death. ASTX295 drives the transition of pancreatic cancer cells from senescence to apoptosis and regulates p53 and DNA damage biomarkers. ASTX295 can be used for the research of hematologic malignancies and pancreatic cancer.

Quinalizarin is a protein kinase CK2 inhibitor with a K_i of 0.052 μM. Quinalizarin exhibits antifungal and anticancer activities. Quinalizarin induces ROS production, apoptotic signaling, mitochondrial pathway activation, cell cycle arrest, and cytotoxicity in cancer cells. Quinalizarin inhibits hyphal growth, biofilm formation, and mature biofilm integrity of Candida albicans. Quinalizarin can be used in research related to cancer and fungal infections.

Euphornin is a anticaner agent, that can be isolated from E. helioscopia. Euphornin induces apoptosis via caspase-mediated pathways. Euphornin induces cell cycle arrest by increasing the level of the phospho-CDK1 (Tyr15) protein.

Gardenin B is a methoxyflavone compound and an inhibitor of USP7, ODC (IC₅₀: 6.24 μg/mL), and Cathepsin D (IC₅₀: 5.61 μg/mL). Gardenin B exhibits antioxidant and antitumor activities. Gardenin B shows IC₅₀ values of 8.87 and 10.59 μg/mL for DPPH and NO scavenging, respectively, and also possesses ferric ion reducing ability. Additionally, Gardenin B can inhibit tumor cell proliferation, induce cell cycle arrest and apoptosis. Gardenin B can be used in cancer research.

Brevetoxin B (Brevetoxin-2) is a red tide toxin. Brevetoxin B affects sodium, potassium and calcium currents in nerve terminals. Brevetoxin B also modulates the metabolic activity of Jurkat cells, reduces cell viability and induces apoptosis. Brevetoxin B can be used in research on synaptic transmission and tumors.

Continentalic acid is a diterpenoid organic acid. Continentalic acid exhibits multiple activities including anti-inflammatory, antioxidant, neuroprotective, antibacterial and antitumor effects. Continentalic acid alleviates oxidative stress, reduces pro-inflammatory cytokine production, inhibits MAPK phosphorylation and neutrophil infiltration, and induces growth inhibition and apoptosis of cancer cells. Continentalic acid can be used in research related to traumatic brain injury, cancer, inflammation and infections.

Sotetsuflavone is a flavonoid that can be isolated from Cycas revolute. Sotetsuflavone inhibits phosphorylation of PI3K, Akt, mTOR, JNK, and p38 MAPK; modulates expression of Cyclin D1, CDK4, Bcl-2, Bax, cleaved caspases 3/9, MMP-9, TGF-β, STAT3, and β-catenin. Sotetsuflavone induces G₀/G₁ cell cycle arrest, apoptosis, autophagy, and intracellular ROS elevation, inhibits cancer cell proliferation. Sotetsuflavone inhibits tumor growth in mouse tumor xenograft models. Sotetsuflavone can be used for the research of non-small cell lung cancer and Crohn’s disease.

6,8-Diprenylorobol, a prenylated isoflavone, is a nature product that could be isolated from the leaves of Cudrania tricuspidata. 6,8-Diprenylorobol antiproliferative effect and induces apoptosis through activation of p53 and generation of ROS.

MKI-3 is a selective microtubule-associated serine/threonine kinase-like (MASTL) inhibitor with an IC₅₀ of 5.72 nM and a K_d of 1.89 nM. MKI-3 disrupts the MASTL-ENSA-Aurora A signaling axis. MKI-3 induces chromosomal instability, mitotic catastrophe and apoptosis (apoptosis) in cancer cells. MKI-3 is applicable to research related to triple-negative breast cancer.

Lacidipine-¹³C₄ is ¹³C labeled Lacidipine (HY-B0347). Lacidipine is an orally active and highly selective L-type calcium channel blocker that acts on smooth muscle calcium channels, primarily dilates peripheral arteries, reduces peripheral resistance, and has long-lasting anti-hypertensive activity. Lacidipine protects HKCs from apoptosis induced by ATP depletion and recovery by modulating the caspase-3 pathway. Lacidipine can be used in studies of hypertension, atherosclerosis and acute kidney injury (AKI).

BLT1-IN-1 is an orally active and selective BLT1 inhibitor with an IC₅₀ of 8.7 nM and a K_d of 121 nM. BLT1-IN-1 exerts protective effects against acute lung injury and sepsis in in vivo models. BLT1-IN-1 can be used in research related to acute lung injury and sepsis.

ZSTK3744 hydrochloride is an aryl hydrocarbon receptor (AhR) agonist. ZSTK3744 hydrochloride directly binds to AhR, upregulates the expression of AhR target genes including CYP1A1, CYP1B1 and TIPARP, and mediates cell growth inhibitory activity in triple-negative breast cancer cells. ZSTK3744 hydrochloride induces apoptosis in triple-negative breast cancer cells. ZSTK3744 hydrochloride exhibits anti-tumor activity and can be used in the research of chemoresistant triple-negative breast cancer.