Caspase Agonist

Phanginin D is a cassane-type furanoditerpene found in the seeds of Caesalpinia sappan. Phanginin D induces apoptosis in HL-60 cells by activating Caspase-3 and promoting the cleavage of procaspase-3 and PARP. Phanginin D can be used for research on human promyelocytic leukemia.

VEGFR-2-IN-70 is a potent VEGFR-2 inhibitor with an IC₅₀ of 18.04 nM. VEGFR-2-IN-70 exhibits cytotoxicity against A549 and MCF-7 cancer cells with IC₅₀ values of 0.43 μM and 3.8 μM, respectively. VEGFR-2-IN-70 induces G1 cell cycle arrest and apoptosis in lung cancer cells. VEGFR-2-IN-70 is useful in cancer research.

TP-110 is a proteasome inhibitor. TP-110 specifically inhibits the protease-like activity of the 20S proteasome, but does not affect the trypsin-like or peptidyl-glutamyl peptide hydrolysis activity. TP-110 inhibits the NF-κB pathway, activates caspase-8, -9, and -3, and causes PARP cleavage, significantly reducing the levels of cIAP-1 and XIAP. TP-110 causes cell cycle arrest at the G2/M phase and promotes apoptosis of cancer cells. TP-110 can be used in cancer research of prostate cancer and multiple myeloma, etc.

STAT3/NF-κB-IN-1 is a potentSTAT3 and NF-κB inhibitor with IC₅₀s of 5.86 (STAT3) and 4.22 μM (NF-κB) in 4T1 cells. STAT3/NF-κB-IN-1 is able to induce apoptosis via its upregulation on key apoptotic regulators; caspases-3/9, Bax and downregulation of Bcl-2. STAT3/NF-κB-IN-1 exerts considerable anticancer activity against breast cancer cell lines and reduces tumor volume in vivo. STAT3/NF-κB-IN-1 can be used for the study of breast cancer.

FAK-IN-28 is an orally active FAK inhibitor (IC₅₀ = 0.4 nM). FAK-IN-28 exhibits dual antiproliferative and anti-metastatic properties. FAK-IN-28 triggers caspase-3-dependent apoptosis via ROS elevation. FAK-IN-28 inhibits tumor growth without causing weight loss or hepatotoxicity. FAK-IN-28 is useful in the study of FAK-driven malignancies, such as colon cancer, cervical cancer, triple-negative breast cancer, and melanoma.

Topoisomerase I/II-IN-1 is a dual inhibitor of topoisomerase I/II. Topoisomerase I/II-IN-1 induces G2/M arrest and apoptosis in cancer cells by upregulating p53, p21, and Bax mRNA levels, caspase-3 protein levels, and the Bax/Bcl-2 ratio, while downregulating Bcl-2. Topoisomerase I/II-IN-1 is useful in the study of various cancers, including melanoma, renal cancer, colorectal cancer, and breast cancer.

HDAC1/6-IN-3 is a potent HDAC inhibitor. HDAC1/6-IN-3 shows excellent inhibitory activities against HDAC1 (IC₅₀ = 1.1 nM) and HDAC6 (IC₅₀ = 2.7 nM). HDAC1/6-IN-3 significantly arrests HepG2 cells at the G0/G1 phase and induces apoptosis and pyroptosis. HDAC1/6-IN-3 exhibits significant antitumor activity in the HepG2 xenograft mode. HDAC1/6-IN-3 can be used for the study of cancers such as liver cancer, lung cancer, colon cancer and breast cancer.

Stigmast-5-en-3-ol induces cancer cell apoptosis and inhibits proliferation by increasing the production of Bax, Caspase-9, p53, and PARP cleavage and reducing Bcl-xl expression. Stigmast-5-en-3-ol exhibits potent inhibitory activity against glucoamylase and α-amylase and possesses high antioxidant activity. Stigmast-5-en-3-ol can be used in the research of diseases such as leukemia, breast cancer, type 2 diabetes, and obesity.

STAT3-IN-44 is a potent STAT3 inhibitor with IC₅₀s of 1.84 (C6 cells) and 4.81 μM (A549 cells). STAT3-IN-44 inhibits STAT3 phosphorylation, downregulates Bcl-2, and upregulates Caspase-3 to promote late-stage apoptosis. STAT3-IN-44 significantly suppresses tumor cell proliferation and migration. STAT3-IN-44 can be used for the study of cancers such as glioma and lung cancer.

Apoptosis inducer 45 is an apoptosis inducer. Apoptosis inducer 45 is cytotoxically active against the MCF-7 cell line. Apoptosis inducer 45 elicits MCF-7 cell apoptosis via the mitochondrial pathway (increases the Bax/Bcl-2 ratio) by activating cleavage of caspase-9, thereby inducing the fragmentation of DNA repair protein PARP. Apoptosis inducer 45 also can induce caspase-8 cleavage, subsequently initiating cleavage of caspase-3 and its downstream protein PARP to culminate in the extrinsic apoptosis. Apoptosis inducer 45 can be used in the research of breast cancer.

Multi-kinase-IN-7 is a multikinase inhibitor with IC₅₀s of 2.19, 2.95, 3.59 and 9.31 μM against EGFR, VEGFR2, TrKA and CDK2, respectively. Multi-kinase-IN-7 shows moderate and weaker activity against FAK, AKT1, GSK3β and CDK5 with IC₅₀ values of 6.3, 9.2, 11.7 and 23.4 μM, respectively. Multi-kinase-IN-7 displays broad spectrum anti­proliferative potential against NCI cancer cell lines. Multi-kinase-IN-7 induces cell cycle arrest, apoptosis and necrosis. Multi-kinase-IN-7 Inhibitor can be used for the study of breast cancer.

SV119 is a selective sigma-2 (σ₂) receptor ligand (K_i ≈ 5-10 nM). SV119 induces apoptosis in various human cancer cell lines by activating caspase-3 and promoting mitochondrial depolarization. SV119 can enhance the effects of chemotherapeutic agents such as Paclitaxel (HY-B0015), increasing their cytotoxicity against tumor cells. SV119 significantly inhibits tumor growth in mouse xenograft models, both alone and in combination. SV119 is useful in the research of cancers such as breast, prostate, and pancreatic cancer.

HDAC-IN-91 is a multiple inhibitor of HDAC (IC₅₀ = 134.22 nM for HDAC1, 66.29 nM for HDAC2), carbonic anhydrase (CA) (K_i = 72.03 nM for CA IX, 50.76 nM for XII), and tubulin polymerization ( IC₅₀ = 2.56 μM). HDAC-IN-91 inhibits PARP1 and increases the Bax/Bcl-2 ratio. HDAC-IN-91 blocks the cell cycle at the G2/M phase and induces apoptosis through a mitochondrial apoptosis activation mechanism. HDAC-IN-91 can exert potent cytotoxic activity through tubulin polymerization inhibition. HDAC-IN-91 can be used in breast, colorectal, cervical and lung cancer research.

Caspase-3 activator 2 (Compound 2f) is a caspase 3 activator that induces apoptosis and can be used in cancer research. Caspase-3 activator 2 is cytotoxic to HL-60 cells and K562 cells, with IC₅₀ values of 33.52 μM and 76.90 μM respectively.

PI3Kδ/HDAC6-IN-1 (Compound 22E) is an orally active and dual inhibitor of PI3Kδ and HDAC6 with IC₅₀ values of 2.4 nM and 6.2 nM, respectively. PI3Kδ/HDAC6-IN-1 exhibits potent antiproliferative effects on non-Hodgkin lymphoma (NHL) cells and possesses in vivo antitumor activity without significant toxicity. PI3Kδ/HDAC6-IN-1 arrests the cell cycle at the G0/G1 phase and induces apoptosis. PI3Kδ/HDAC6-IN-1 blocks the PI3K/AKT/mTOR signaling pathway and increases the acetylation levels of α-tubulin and histone H3.

STAT3/CAIX-IN-1 is a dual-target inhibitor of STAT3 (K_d: 60.03 μM) and CAIX (IC₅₀: 80.45 nM). STAT3/CAIX-IN-1 induces ferroptosis by increases the levels of reactive oxygen species (ROS) and lipid peroxides. STAT3/CAIX-IN-1 inhibits cell migration, induces apoptosis, and causes cell cycle arrest in MDA-MB-231 cells. STAT3/CAIX-IN-1 can be used for the study of triple-negative breast cancer (TNBC).

p38α inhibitor 6 (compound 19) is a p38α inhibitor with the IC₅₀ of 0.68 μM. p38α inhibitor 6 induces cell apoptosis and arrests cell cycle at G0 and G2/M phase. p38α inhibitor 6 decreases the TNF-α concentration as well as increased the expression of tumor suppressor gene p53, Bax/BCL-2 ratio and caspase 3/7.

HDAC-IN-93 is a HDAC inhibitor with promising total pan-HDAC inhibitory activity. HDAC-IN-93 demonstrates significant broad-spectrum antiproliferative activity across various cancer cell lines. HDAC-IN-93 induces cell apoptosis along with necrosis. HDAC-IN-93 can be used for the studies of prostate cancer and breast cancer.

MMP-9-IN-14 is a MMP-9 inhibitor (IC₅₀ = 34.46 μM). MMP-9-IN-14 induces G1-phase cell cycle arrest and caspase-dependent apoptosis in cancer cells. MMP-9-IN-14 promotes the accumulation of phosphorylated γH2AX. MMP-9-IN-14 inhibits the migration and invasion of cancer cells, and downregulates the expressions of MMP-2, MMP-9 and hTERT in cancer cells. MMP-9-IN-14 inhibits tumor growth and angiogenic spread in animal models. MMP-9-IN-14 can be used for the research of cancers such as lung adenocarcinoma, cervical cancer and colorectal cancer.

4-Methoxycinnamic acid ethyl ester (Ethyl p-methoxycinnamate) is an orally active natural compound found. 4-Methoxycinnamic acid ethyl ester exerts anti-inflammatory effects by inhibiting cyclooxygenase (COX-1 (IC₅₀ = 1.12 μM) and COX-2 (IC₅₀ = 0.83 μM)), NF-κB (IC₅₀ = 88.7 μM) and cytokine production (TNF-α (IC₅₀ = 96.84 μg/mL) and IL-1β (IC₅₀ = 166.4 μg/mL)). 4-Methoxycinnamic acid ethyl ester inhibits tumor cell proliferation, migration and cancer metabolism and induces apoptosis.4-Methoxycinnamic acid ethyl ester inhibits VEGF expression, thereby inhibiting angiogenesis. 4-Methoxycinnamic acid ethyl ester has a significant inhibitory effect on dengue virus and Mycobacterium tuberculosis. 4-Methoxycinnamic acid ethyl ester has analgesic effects in rats.