Apoptosis Inducer

Panobinostat-d₄ is the deuterium labeled Panobinostat. Panobinostat (LBH589; NVP-LBH589) is a potent and orally active non-selective HDAC inhibitor, and has antineoplastic activities[1][2]. Panobinostat induces HIV-1 virus production even at low concentration range 8-31 nM, stimulates HIV-1 expression in latently infected cells[4]. Panobinostat induces cell apoptosis and autophagy. Panobinostat can be used for the study of refractory or relapsed multiple myeloma[3].

Galgravin is an active compound in Nectandra megapotamica, with anti-inflammatory activity. Galgravin displays in vitro cytotoxic activity and induce apoptosis in leukemia cells.

HDAC3/6-IN-2 (compound 15) is a potent HDAC6 and HDAC3 inhibitor, with IC₅₀ values of 0.368 and 0.635 μM, respectively. HDAC3/6-IN-2 shows antitumor activity, and induces cancer cell apoptosis. HDAC3/6-IN-2 decreases the levels of HDAC6 and HDAC3, associated with upregulation of acetylated H3 and α-tubulin.

Topoisomerase II/EGFR-IN-2 (Compound 3) is an inhibitor of Topoisomerase IIα (IC₅₀ = 0.122 μM) and EGFR-TK^WT (IC₅₀ = 16.8 μM). Topoisomerase II/EGFR-IN-2 inhibits the proliferation of HeLa and HepG2 cells, inducing cell cycle arrest and apoptosis. Topoisomerase II/EGFR-IN-2 upregulates caspase-3 and Bax, and downregulates Bcl-2. Topoisomerase II/EGFR-IN-2 can be used to study liver cancer and cervical cancer.

Anticancer agent 136 (compound 22), a C17-triazole analogue of Geldanamycin (GDM; HY-15230), has an IC₅₀ of 3.38 μM for HDF and a K_d of 3.86 μM for Hsp90. Anticancer agent 136 is an apoptosis-inducing agent.

EGFR-IN-96 (compound 7a) is a thieno[2,3-d]pyrimidine EGFR inhibitor that can induce apoptosis. EGFR-IN-96 arrests the growth of HepG2 cells in the S phase and G2/M phase, and inhibits the growth of cancer cells bearing EGFR wild-type and EGFR^T790M.

ZLHQ-5f is a dual CDK2 and Topo I inhibitor with an IC₅₀ of 0.145 μM against CDK2/CycA2. ZLHQ-5f arrests the cell cycle in S-phase, triggers apoptosis in HCT116 cells, and has a good safety profile.

dCASP1-55 is a cereblon-dependent caspase-1 (CASP1) PROTAC degrader. dCASP1-55 induces excessive NF-κB activation, apoptosis, and moderate S-phase arrest in leukemic cells. dCASP1-55 suppresses colony formation of leukemic cells. dCASP1-55 can be used for the research of cancer, such as myeloid malignancies and acute myeloid leukemia.

SeSA-HCPT is an orally active dual-target inhibitor integrating Topo I and HDAC inhibition. SeSA-HCPT induces potent DNA damage, apoptosis, S-phase arrest in prostate cancer cells. SeSA-HCPT inhibits cancer cells proliferation and migration. SeSA-HCPT impairs homologous recombination by suppressing KIF4A-RAD51 signaling. SeSA-HCPT markedly inhibits CRPC tumor growth with minimal systemic toxicity.

Thalidomide-5-NH-PEG6-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-5-NH-PEG6-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.

PKMYT1-IN-10 is a selective PKMYT1 inhibitor with an IC₅₀ of 3 nM. PKMYT1-IN-10 inhibits colony formation, induces apoptosis, and induces S-phase cancer cell cycle arrest. PKMYT1-IN-10 exhibits liver microsomal stability, favorable plasma stability, minimal CYPs inhibition. PKMYT1-IN-10 can be used for the studies of ovarian cancer and breast cancer.

3-Fluoro-evodiamine glucose (Compound 8) is an evodiamine-glucose conjugate. 3-Fluoro-evodiamine glucose activates the expression of glucose transporter 1 (GLUT1), and inhibits topoisomerase I/II. 3-Fluoro-evodiamine glucose induces apoptosis and arrests the cell cycle at G2/M phase. 3-Fluoro-evodiamine glucose exhibits antitumor efficacy in vivo and in vitro, without significant toxicity.

Silydianin (Standard) is the analytical standard of Silydianin (HY-N0646). This product is intended for research and analytical applications. Silydianin is a flavonolignan. Silydianin can be obtained from Silybum marianum. Silydianin inhibits PTP1B with an IC₅₀ of 17.38 μM. Silydianin inhibits both monophenolase and diphenolase of tyrosinase significantly, with IC₅₀s of 2.6 μM and 16.5 μM, respectively. Silydianin induces Apoptosis and reduces cytokines (IL-4 and IL-5). Silymarin has antioxidant, cytoprotective and immunomodulatory effects. Silydianin has antitumor activity against prostate cancer. Silymarin can be used in allergic asthma research.

(E)-Ethyl p-methoxycinnamate (Standard) is the analytical standard of (E)-Ethyl p-methoxycinnamate. This product is intended for research and analytical applications. (E)-Ethyl p-methoxycinnamate is a natural product found in Kaempferia galangal with anti-inflammatory, anti-neoplastic and anti-microbial effects. (E)-Ethyl p-methoxycinnamate inhibits COX-1 and COX-2 in vitro with IC₅₀s of 1.12 and 0.83 μM, respectively.

KRAS G12D-IN-37 is a KRAS^G12D inhibitor. KRAS G12D-IN-37 shows antiproliferative activity against KRAS^G12D mutant tumor cells and minimal cytotoxicity toward normal cells. KRAS G12D-IN-37 binds stably to KRAS^G12D via hydrogen bond interactions with residues His 95, Arg 68, and Asp 12, and inhibits downstream ERK/AKT signaling pathways. KRAS G12D-IN-37 elevates ROS levels, induces apoptosis, disrupts mitochondrial membrane potential. KRAS G12D-IN-37 downregulates the level of anti-apoptotic protein Bcl-2, and upregulates the levels of pro-apoptotic proteins Bax and caspase 3. KRAS G12D-IN-37 can be used for the research of cancer, such as gastric adenocarcinoma and colorectal cancer.

VEGFR-2-IN-61 (Compound 7b) is an inhibitor for VEGFR-2 with an IC₅₀ of 2.83 µM. VEGFR-2-IN-61 inhibits the proliferation of multi cancer cells (IC₅₀ for MCF-7 is 2.12 μM). VEGFR-2-IN-61 inhibits the cell migration, induces oxidative stress and apoptosis in MCF-7.

TAT-327 is cell-penetrating peptide. TAT-327 selectively inserts into cancer cell membranes and shows potent antitumor activity. TAT-327 effectively inhibits cancer cells proliferation, induces apoptosis and disrupts EGFR signal pathway by inhibiting downstream signals (such as IL-2, TNF-α and IFN-γ) expression and the Eps8/EGFR interaction. TAT-327 significantly inhibits tumor growth in HT-29 xenograft mcie models.

HBF-0079 is a selective anti-hepatocellular carcinoma agent. HBF-0079 induces cell cycle arrest and Apoptosis. HBF-0079 modulates cell-growth and anti-apoptotic signaling through AKT and mTOR. HBF-0079 exhibits antitumor activity against hepatocellular carcinoma.

Aurora kinase/ALK-IN-1 is a dual Aurora A kinase and ALK inhibitor with IC₅₀ values of 0.296 μM and 0.332 μM, respectively. Aurora kinase/ALK-IN-1 induces G₂/M cell cycle arrest, triggers mitochondrial apoptosis, elevates intracellular reactive oxygen species (ROS) levels, and inhibits ALDH1 activity. Aurora kinase/ALK-IN-1 demonstrates cytotoxicity and tumor selectivity. Aurora kinase/ALK-IN-1 can be used for the research of anaplastic large cell lymphoma.

PROTAC AURKA degrader-4 is a AURKA PROTAC degrader with a DC₅₀ of 25.62 nM (Jurkat cells). PROTAC AURKA degrader-4 recruits the CRBN E3 ubiquitin ligase via the ubiquitin-proteasome system. PROTAC AURKA degrader-4 disrupts both the catalytic and non-catalytic functions of AURKA, including its interactions with TPX2 and c-Myc. PROTAC AURKA degrader-4 induces G2/M phase arrest and apoptosis. PROTAC AURKA degrader-4 exhibits enhanced antiproliferative activity and in vivo antitumor efficacy in models with high CRBN and AURKA expression. PROTAC AURKA degrader-4 can be used for the research of acute lymphoblastic leukemia.