Apoptosis Inducer

SAR442085 is an Fc-engineered anti-CD38 monoclonal antibody with a K_d of 0.2 nM for human CD38. SAR442085 inhibits CD38, induces apoptosis, and triggers antibody-dependent cellular cytotoxicity and phagocytosis in CD38-expressing tumor cells. SAR442085 binds allelic variants of FcγRIIa and FcγRIIIa, enhances NK cell activation, degranulation and cytokine secretion, and exerts anti-tumor activity in human Fc receptor transgenic mice. SAR442085 can be used in the research of multiple myeloma.

GR2-128 is a dual inhibitor targeting MLK3 and NAMPT with IC₅₀ values of 84 nM and 14 nM, respectively. GR2-128 inhibits downstream JNK/c‑Jun signaling and reduces NAD⁺ levels. GR2-128 exhibits antiproliferative and pro-apoptotic activities in triple-negative breast cancer cells without significant toxicity to normal cells. GR2-128 suppresses tumor growth, reduces macrophage and neutrophil infiltration, and increases tumor T-cell markers in a syngeneic mouse model, and can be used for triple-negative breast cancer research.

PROTAC EGFR degrader 6 is a PROTAC-based degrader and inducer targeting EGFRdel19. PROTAC EGFR degrader 6 induces the degradation of EGFRdel19 via the ubiquitin-proteasome system. PROTAC EGFR degrader 6 induces apoptosis. PROTAC EGFR degrader 6 arrests cells at the G1 phase. PROTAC EGFR degrader 6 can be used in research related to non-small cell lung cancer.

[1,1′:4′,1′′-Terphenyl]-3,4′′,5-triol (compound 13g) is a terphenyl derivative that blocks the cell cycle in the G0-G1 phase and induces differentiation in leukemia cells. [1,1′:4′,1′′-Terphenyl]-3,4′′,5-triol shows a potent apoptotic effect.

Antiangiogenic agent 6 (Pt-1) can inhibit angiogenesis. Antiangiogenic agent 6 can induce necroptosis in tumor cells.

TAT-N24 is a cell-penetrating peptide and also an inhibitor of p55PIK. TAT-N24 disrupts the interactions between p55PIK and p53, PCNA or Rb, blocks the p53-dependent ubiquitin-mediated degradation process, and inhibits the nuclear translocation and phosphorylation of NF-κB p65. TAT-N24 enhances MMS-induced p53-dependent cell apoptosis, inhibits DNA synthesis, reduces the expression of Cyclin D1, and induces cell cycle arrest at the G0/G1 or S phase. TAT-N24 inhibits the activation of NLRP3 and NLRC4 inflammasomes, reduces the expression of ZBP1-PANoptosome components, and suppresses PANoptosis. TAT-N24 can be used in research related to leukemia, colon cancer, cervical cancer, liver cancer, corneal neovascularization, restenosis and acute glaucoma.

Delphinidin 3-glucoside (chloride) (Standard) is the analytical standard of Delphinidin 3-glucoside (chloride). This product is intended for research and analytical applications. Delphinidin 3-glucoside chloride (Delphinidin 3-O-glucoside chloride) is an active anthocyanin found in Hibiscus sabdariffa extract. Delphinidin 3-glucoside chloride induces a pro-apoptotic effect in B cell chronic lymphocytic leukaemia (B CLL). Delphinidin 3-glucoside chloride exerts phytoestrogen activity by binding to ERβ, with an IC50 of 9.7 μM. Delphinidin-3-O-glucoside chloride inhibits EGFR with an IC50 of 2.37 µM. Delphinidin 3-glucoside chloride exhibits antitumor effects through pAKT/IRF1/HOTAIR pathway. Delphinidin 3-glucoside chloride exhibits efficacy against oxidative stress, inhibits platelet activation and endothelial dysfunction.

MET/PDGFRA-IN-2 (compound 8h) is a MET and PDGFRA protein inhibitor. MET/PDGFRA-IN-2 induces cell apoptosis. MET/PDGFRA-IN-2 inhibits proliferation of MET-positive cells (IC₅₀s: 9.7, 6.1, 12.0, 11.5, 8.6, 34.4 μM for AsPc-1, EBC-1, MKN-45, Mia-Paca-2, HT-29, K562 cells respectively).

AGW-11 is a potent dual inhibitor of EGFR (IC₅₀ = 556 nM) and VEGFR2 (IC₅₀ = 289.7 nM). AGW-11 induces apoptosis and suppresses phosphorylation of EGFR, VEGFR2, and ERK1/2 in HUVECs. AGW-11 effectively inhibits cancer cell growth, reduces HUVEC proliferation, tube formation, and invasion, thereby blocking angiogenesis. AGW-11 significantly suppresses tumor growth and decreases lung metastasis in a 4T1 xenograft mouse model. AGW-11 can be used for the study of breast cancer.

Aspirin calcium is an orally active, potent and irreversible inhibitor of cyclooxygenase COX-1 and COX-2, with IC₅₀ values of 5 and 210 μg/mL, respectively. Aspirin calcium induces apoptosis. Aspirin calcium inhibits the activation of NF-κB. Aspirin calcium also inhibits platelet prostaglandin synthetase, and can prevent coronary artery and cerebrovascular thrombosis.

Lepidozin G inhibits the growth of a panel of cancer cell lines with IC₅₀ values ranging from 4.2 ± 0.2 to 5.7 ± 0.5 μM. Lepidozin G induces PC-3 cell death via mitochondrial-related apoptosis.

CSF1R-IN-22 (Compound C19) is an orally effective CSF-1R selective inhibitor (IC₅₀<6 nM). CSF1R-IN-22 enhances the secretion of CXCL9 from M2 macrophages, increases CD8⁺ T cell infiltration. CSF1R-IN-22 boosts anti-tumor immune responses of anti-PD-1, and induces apoptosis in tumor cells. CSF1R-IN-22 can effectively reprogram M2-like TAMs (tumor-associated macrophages) to the M1 phenotype and reshape the TME by inducing the recruitment of CD8⁺ T cells into tumors and reducing the infiltration of immunosuppressive Tregs and MDSCs.

Thalidomide-O-C4-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.

Dienogest-d₅ is deuterium labeled Dienogest.

Thalidomide-2,6-diazaspiro[3.4]octane-C-Pip-boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Thalidomide-2,6-diazaspiro[3.4]octane-C-Pip-boc can serve as a Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.

HDAC-IN-42 (compound 14f) is a potent and selective HDAC inhibitor with IC₅₀ values of 0.19 and 4.98 µM for HDAC1 and HDAC6, respectively. HDAC-IN-42 shows anticancer and anti-proliferative activity. HDAC-IN-42 induces apoptosis and cell cycle arrest at G2/M phase.

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.

AX8819 is a selective dipeptidyl peptidase II (DPP II) inhibitor with an IC₅₀ of 0.88 nM. AX8819 induces caspase-dependent apoptosis. AX8819 exhibits low non-specific toxicity toward proliferating T cells. AX8819 can be used for the research of B cell chronic lymphocytic leukemia.

HDAC-IN-9 is a potent and selective tubulin and HDAC dual inhibitor. HDAC-IN-9 inhibits the invasion and migration of A549 cells. HDAC-IN-9 shows potent antitumor and antiangiogenic effect in vitro and in vivo.

DIX-01 is a CRBN-recruiting molecular glue and cytotoxic agent targeting GSPT1, with an EC₅₀ of 173 nM against human GSPT1. DIX-01 drives proteasomal degradation of GSPT1, IKZF1 and IKZF3, and induces cytotoxicity in cancer cells. DIX-01 inhibits tumor growth in a zebrafish xenograft model and can be used for research on acute myeloid leukemia and prostate cancer.