Apoptosis

<p>Cadonilimab (AK104) is a tetravalent PD-1/CTLA-4 bispecific humanised antibody that activates T cells by enhancing IL-2 and IFN-γ secretion.</p>

<p>Fosinopril, a prodrug ACE inhibitor for hypertension, converts to active fosinoprilat.</p>

<p>Dalotuzumab (MK-0646) is an anti-IGF-1R mAb that inhibits oncogenic signaling, inducing tumor cell apoptosis.</p>

<p>Triethanolamine oleate is a nonionic surfactant</p>

<p>Afimkibart (PF06480605) is a humanised monoclonal antibody targeting TL1A (TNF-like Ligand 1A), which blocks TL1A-DR3 (death domain receptor 3) signalling on restrictive immune cells and fibroblasts. It can be used for inflammatory bowel disease and ulcerative colitis.</p>

<p>Tabalumab (LY2127399) is a humanised monoclonal antibody targeting BAFF that neutralises both soluble and membrane-bound forms of BLyS , autoimmune diseases.</p>

<p>Peresolimab is a humanized antibody targeting PD-1, potentially stimulating immune inhibitory pathways for autoimmune disease research.</p>

<p>Sugemalimab: human anti-PD-L1 IgG4 mAb with anticancer properties for non-small cell lung cancer.</p>

<p>Azintuxizumab, an IgG4 bispecific antibody, targets BCMA, offering dual-action immunotherapy for relapsed/refractory multiple myeloma in preclinical studies.</p>

<p>Microtubule Inhibitor 8 (MP-HJ-1b) serves as a potent disruptor of microtubule function, inducing cell death via ferroptosis and demonstrating anti-tumor effects [1] [2].</p>

<p>Visilizumab is a humanized anti-CD3 IgG2 mAb with low Fc binding, modulating T-cell function for ulcerative colitis and Crohn's.</p>

<p>Frexalimab (SAR441344; INX-021), a monoclonal antibody that targets the CD40 ligand (CD40L), shows promise for research in multiple sclerosis [1].</p>

<p>Bleselumab (ASKP 1240) is a humanised monoclonal antibody targeting CD40, inhibiting immune responses, organ transplant rejection.</p>

<p>Ravagalimab (ABBV-323) is a CD40 antagonist monoclonal antibody, investigated for Crohn’s disease and Sjögren’s syndrome to evaluate immune modulation.</p>

<p>Rosnilimab is a PD-1 agonist that inhibits T cell proliferation and depletes T cells, enabling research into inflammatory diseases.</p>

<p>Neihulizumab is an anti-CD162 antibody that induces apoptosis in activated T cells for treating GVHD and psoriasis.</p>

<p>AHR agonist 3 is an agent with therapeutic activity.</p>

<p>Geptanolimab (CBT-501) is a humanized IgG4κ antibody against PD-1, blocking PD-L1/PD-L2 binding to reactivate T cell activity.</p>

<p>Cosibelimab, a fully human monoclonal antibody, blocks PD-L1, enabling ADCC and CDC against cancer cells.</p>

<p>Afelimomab (MAK 195F), a F(ab')2 fragment of an anti-tumor necrosis factor monoclonal antibody, is utilized in sepsis research [1].</p>

<p>Tagitanlimab (HBM-9167) is a humanized IgG1κ anti-PD-L1 antibody, potentially for recurrent/metastatic NPC.</p>

<p>Vonsetamig, a humanized immunoglobulin G4-kappa monoclonal antibody, targets both TNFRSF17 and CD3E. It serves as an antineoplastic agent.</p>

<p>Linvoseltamab, a bispecific antibody, targets both BCMA (TNFRSF17) and CD3 epsilon, demonstrating a favorable safety profile and promising efficacy in relapsed/</p>

<p>Inezetamab is a bispecific anti- CD40 and anti- MSLN IgG1 monoclonal antibody [1] .</p>

<p>Reozalimab (LY3434172) is a bispecific monoclonal antibody targeting PD-1/PD-L1, antitumour and enhances T-cell activation in vitro.</p>

<p>Toralizumab: humanized mAb targeting CD40L to curb T cell signaling and explore SLE treatment.</p>

<p>Visugromab (CTL-002) is a monoclonal antibody that targets and neutralises GDF-15.</p>

<p>Amantadine: antiviral, anti-Parkinson's, blocks NMDA receptors, boosts dopamine/norepinephrine release.</p>

<p>Benazepril inhibits the activity of circulating angiotensin-converting enzyme (ACE) in horses.</p>

<p>RMC5127 is an oral and mutation-selective inhibitor of RASG12V (ON) that inhibits the GTP-bound (ON) form of RAS G12V with CNS and brain permeability.</p>

<p>Toripalimab is a humanized anti-PD-1 monoclonal antibody used as an immune checkpoint inhibitor in research for advanced malignancies like nasopharyngeal carcinoma.</p>

<p>Cifurtilimab (SEA-CD40) is a humanised monoclonal antibody acting as a CD40 agonist. It enhances binding to activated FcγRIIIa, anticancer.</p>

<p>Ivuxolimab is a human IgG2 antibody that acts as an OX40 agonist, promoting T cell responses for anti-tumor immunity research.</p>

<p>Pucotenlimab (HX008) is an anti-PD-1 mAb that blocks PD-1/PD-L1/2 interactions, restoring immune function against solid tumours.</p>

<p>Tecaginlimab (BNT-312), an Fc-inert bispecific antibody, targets CD40/4-1BB to boost tumor immunity.</p>

<p>Vudalimab: humanized antibody, blocks PD-1 &amp; CTLA-4, boosts selective T-cell tumor response.</p>

<p>Anti-Mouse TNFR2 Antibody is an Armenian Hamster-derived IgG inhibitor specifically targeting mouse TNFR2.</p>

<p>potent p53 inhibitor</p>

<p>Remtolumab (ABT-122) is a dual inhibitor of TNFα and IL-17A for rheumatoid arthritis research.</p>

<p>Licaminlimab (OCS-02) is a single-chain antibody fragment targeting TNF alpha, an inflammatory cytokine.</p>

<p>Tuvonralimab, a combo of anti-PD-1/IgG4 and anti-CTLA-4/IgG1 antibodies, blocks dual immune checkpoints.</p>

<p>Acasunlimab (GEN1046) is a bsAb that targets PD-L1 and 4-1BB, boosting T/NK cells and blocking PD-1/PD-L1 in cancer research.</p>

Galanthamine-O-methyl-d3 is a deuterated compound of Galanthamine-O-methyl. Galanthamine-O-methyl has a CAS number of 357-70-0. Galanthamine is an acetylcholinesterase (AChE)inhibitor(IC50 : 500 nM), can reduce brain damage induced by hypoxia-ischemia.

<p>Stavudine-α,α,α,6-d4 is a deuterated compound of Stavudine. Stavudine has a CAS number of 3056-17-5. Stavudine, a nucleoside reverse transcriptase inhibitor analog of thymidine, has activity against HIV.</p>

<p>Meloxicam D4: deuterium-labeled, non-steroidal anti-inflammatory; COX-1 inhibitor (IC50: 36.6μM), COX-2 inhibitor (IC50: 0.49μM).</p>

<p>Dasatinib D8 is deuterium-labeled dasatinib. Dasatinib is a dual Bcr-Abl and Src family tyrosine kinase inhibitor.</p>

<p>Limonin glucoside: a citrus compound, blocks HIV/HTLV-1, triggers cancer cell death, kills Aedes larvae.</p>

<p>Propylparaben-d4 is a deuterated compound of Propylparaben. Propylparaben has a CAS number of 94-13-3. Propylparaben is an antimicrobial agent, preservative, flavouring agent</p>

<p>Pioglitazone D4 is a deuterium labeled Pioglitazone. Pioglitazone is a agonist of PPARγ .</p>

<p>5'-Deoxy-5'-methylthioadenosine-d3 is a deuterated MTA analog used as an internal standard in metabolomic studies.</p>

<p>Ionomycin calcium (SQ23377 calcium) is an effective and selective calcium ionophore, exhibiting high specificity for calcium ions. Cost-effective and quality-assured.</p>

<p>CPTH6, a thiazole derivative, selectively inhibits the lysine acetyltransferase activity of Gcn5 and pCAF without affecting p300 or CBP. It effectively blocks the acetylation of H3/H4 histones and α-tubulin in various leukemia cell lines, leading to reduced cell viability by arresting the cell cycle in the G0/G1 phase and inducing apoptosis. Additionally, CPTH6 disrupts autophagy across several tumor cell lines, primarily by interfering with ATG7-mediated autophagosomal membrane elongation.</p>

<p>Prosultiamine is commonly used for treatment of beriberi, nutritional disorders caused by lack of vitamin B1, etc.</p>

<p>IA-14069 is a TNF-a inhibitor with anti-inflammatory activity and pro-inflammatory cytokine production, and is used in the study of colon cancer.</p>

<p>p-Decylaminophenol is a melanogenesis inhibitor.</p>

<p>Talaporfin is a photosensitizer used in photodynamic therapy.</p>

<p>GZD856 formic inhibits PDGFRα/β (IC50: 68.6, 136.6 nM) &amp; Bcr-Abl (IC50: 19.9, 15.4 nM), with antitumor properties.</p>

<p>Avenanthramide A is a biochemical.</p>

Esmolol is a cardioselective beta-blocker used in parenteral forms in the treatment of arrhythmias and severe hypertension.

<p>Diethylamiodarone is the main metabolite of amiodarone in vivo.</p>

<p>Quinacrine methanesulfonate is a bioactive chemical.</p>

<p>EGFR-IN-109 (compound 4), an EGFR inhibitor, displays IC 50 values of 25.8 nM for EGFR WT and 182.3 nM for EGFR T790M. This compound halts the growth of cancer cells at the G2/M phase and triggers both early and late apoptosis. It is applicable in cancer research [1].</p>

<p>4-(6-Bromo-2-benzothiazolyl)benzenamine is a β-amyloid PET tracer and can be used in the diagnosis of neurological diseases.</p>

<p>MCL-1/BCL-2-IN-2 (Compound Nap-1) is a potent and selective dual inhibitor of Mcl-1 and Bcl-2 with IC 50 s of 4.45 and 3.18 μM, respectively [1].</p>

<p>Zibotentan (ZD4054) (ZD4054) is a specific Endothelin (ET)A antagonist with IC50 of 21 nM, exhibiting no activity at ETB. Phase 3.</p>

<p>Diquafosol Free Base is a purinoceptor P2Y(2) receptor agonist.</p>

<p>EGFR-IN-117 (Compound 8h) exhibits inhibitory activity against EGFR mutations, specifically targeting the tumor environment and inducing apoptosis in cancer cells. This compound effectively inhibits the proliferation of H1975, PC-9, and mutant EGFR cells including BaF3-EGFRL858R/T790M/C797S and BaF3–C797S/Del19/T790M, with IC50 values of 13 nM, 19 nM, 1.2 nM, and 1.3 nM respectively. Additionally, EGFR-IN-117 demonstrates anti-tumor activity in mouse models.</p>

<p>SM1044 is a dimer of dihydroartemisinin (DHA). It activates caspase, inducing apoptosis in RL95-2 and KLE cells. SM1044 inhibits the proliferation of cancer cells RL95-2, KLE, HEC-50, HEC-1-A, HEC-1-B, and AN3CA, with an IC50 of less than 3.6 μM. Additionally, SM1044 suppresses tumor growth in RL95-2 xenograft mouse models.</p>

<p>Asobamast is a biochemical.</p>

<p>nor-NOHA acetate (Nω-Hydroxy-nor-L-arginine acetate) is a reversible inhibitor of arginase, with anti-leukemic activity, effective in endothelial dysfunction,</p>

<p>Dalbinol is a useful organic compound for research related to life sciences. The catalog number is T124857 and the CAS number is 41993-79-7.</p>

<p>Kaolin (Bolus alba) is a clay dominated by minerals of the kaolinite family. Kaolin increased the sensitivity of this method for monitoring hemophilia therapy.</p>

<p>AC-4-130 inhibits STAT5 SH2 domain, blocks gene transcription, induces apoptosis in FLT3-ITD leukemia, and shows anti-AML potential.</p>

<p>Xevinapant hydrochloride (AT-406 HCl) , an orally active antagonist of multiple inhibitor of apoptosis proteins(IAP), inhibits progression of human ovarian Y binding to XIAP-BIR3, cIAP1-BIR3 and cIAP2-BIR3 with Ki of 66.4 nM, 1.9 nM, and 5.1 nM, 50- to 100-fold higher affinities than the Smac AVPI peptide.</p>

<p>Applications (3S,4S)-(+)-1-Benzyl-3,4-pyrrolidinediol is used as a reagent in organic synthesis including that of pyrrolidine iminocyclitol α-glucosidase inhibitors and (-)-(1R,2R,7S,8aR)-1,2,7-Trihydroxyindolizidine ((-)-7S-OH-Lentiginosine) which has potential proapoptotic properties.<br>References Guerreiro, L., et al.: Bioorg. Med. Chem., 21, 1911 (2013); Cordero, F., et al.: ChemPlusChem, 77, 224 (2012);<br></p>

<p>Applications 4-Methyl-1H-imidazole-5-carboxylic Acid is used in preparation of Cyclohexyl Benzamide compounds for treatment of type II diabetes. Also, used in preparation of Triazolylphenyl substituted Amides as apoptosis signal-regulating kinase inhibitors.<br>References Hu, Z., et al.: PCT Int. Appl.,(2018); Corkey, B., et al.: U.S., (2015);<br></p>

<p>Applications Selonsertib is an apoptosis signal-regulating kinase 1 (ASK1) inhibitor with potential anti-inflammatory, antineoplastic and anti-fibrotic activities. Selonsertib interacts with the catalytic kinase domain of ASK1 and prevents its phosphorylation and activation. As a result, the expression of genes involved in fibrosis, cellular proliferation, and apoptosis are down regulated.<br>References Nelson, C. H. et al.: Clin Pharmacol Ther. 98, 630 (2015); Lin, J. H., et al.: Nephron. 129, 29 (2015)<br></p>

<p>Stability Hygroscopic<br>Applications Ginsenoside F2 is a bioactive metabolite of the ginsenoside component of Panax ginseng with the ability to regulate element-binding protein cleavage activating protein and transforming growth factor-β pathways. This control over apoptosis can lead to a control over hair growth and hair loss in mammals.<br>References Shin, H. et al.: Biol. Pharm. Bull., 37, 755 (2014); Shin, H. et al.: Eur. J. Pharm., 730, 82 (2014);<br></p>

<p>Applications Mollugin is an anti-tumor agent inducing apoptosis and autophagy in various cancer models.<br>References Zhang, L. et al.: Biochem. Biophys. Res. Comm., 450, 247 (2014); Idhayadhulla, A. et al.: Bioorg. Chem., 52, 77 (2014);<br></p>

<p>Stability Hygroscopic<br>Applications MelittinTrifluoroacetic Acid Salt is the Trifluoroacetic Acid Salt version of Melittin which is an apoptosis inducer, a NF-κB inhibitor, and a PLA2 activator.<br>References Han, S., et al.: J Asian Nat Prod Res. 11, 796-804 (2009); Park, C., et al.: Biochem. Biophys. Res. Commun., 394, 170-172 (2010); Park, J.H., et al.: Mol. Cells., 29, 209-215 (2010);<br></p>

<p>Applications Graveoline is an apoptosis and autophagy inducer in skin melanoma cancer cells.<br></p>

<p>Applications Pyocyanin is an antibiotic accelerator of neutrophil apoptosis.<br></p>

<p>Applications Apogossypolone is an anticancer agent that induces apoptosis in carcinoma cells. Antiproliferative.<br>References Zubair, H. et al.: Eur J. Pharm. Sci., 47, 280 (2012);<br></p>

<p>Applications tert-Butyl 4-Bromo-2-fluorobenzoate is an intermediate of enzalutamide (M199800). Enzalutamide is an androgen-receptor antagonist that blocks androgens from binding to the androgen receptor and prevents nuclear translocation and co-activator recruitment of the ligand-receptor complex. MDV 3100 has also been shown to induce tumor cell apoptosis, and has no agonist activity. MDV 3100 is a candidate for the treatment of castration-resistant prostate cancer.<br>References Scher, H.I. et al.: Lancet, 375, 1437 (2010); Bellmunt, J. et al.: Ther. Adv. Med. Oncol., 2, 189 (2010); Ryan, C.J. et al.: J. Clin. Oncol., 29, 3651 (2011);<br></p>

<p>Applications N-(Ethoxycarbonylmethyl)piperazine is used in the preparation of aralkylpiperazine- and aryl-substituted hydrazines, particularly benzylpiperazineacetyl hydrazones of hydroxyaryl aldehydes, as selective inducers of apoptosis and activators of procaspases for use as anticancer agents.<br>References Nakagawara, A., et al.: Cancer Res., 57, 4578 (1997), Denault, J., et al.: J. Biol. Chem., 278, 34042 (2003), Traven, A., et al.: Cancer Cell, 5, 107 (2004), Becattini, B., et al.: Chem. Biol., 11, 389 (2004),<br></p>

<p>Applications An analogue of Olomoucine (Cat. # O567000) that acts as a potent inhibitor of Cdk 1 (IC50=100nm) and Cdk2 (IC50=80nm). Also displays antiproliferative and proapoptotic effects.<br>References Wermeulen, K., et al.: Leukemia, 16, 299(2002)<br></p>

<p>Applications Intermediate in the production of cell death regulators and apoptosis promoters.<br></p>

<p>Applications Ceramide-1-phosphate blocks apoptosis through inhibition of acid sphingomyelinase in macrophages.<br></p>

<p>Applications Aurintricarboxylic Acid is a cell-permeable apoptosis inhibitor.<br></p>

<p>Applications Santamarine is a sesquiterpene lactone shows anticancer properties by inhibiting proliferation and inducing apoptosis.<br>References Mehmood, T., et al.: J. Cancer, 8, 1-11 (2017)<br></p>

<p>Stability Hygroscopic<br>Applications Delanzomib is an orally active proteasome inhibitor. Delanzomib has been shown to down-modulate NF-κB, induce apoptosis, inhibit angiogenesis and M-CSF-RANKL-induced osteoclastogenesis.<br>References Piva, R. et al.: Blood, 111, 2765 (2008); Sanchez, E. et al.: Br. J. Haematol., 148, 569 (2010);<br></p>

<p>Stability Hygroscopic<br>Applications A potent and selective ATP-competitive dual inhibitor cdc7/cdk9. It blocks DNA synthesis and affects the phosphorylation of the replicative DNA helicase at Cdc7-dependent phosphorylation sites. Inhibits cell proliferation in a variety of human cell lines and induces apoptosis in a p53-independent manner in vivo. Also inhibits mitogen-activated protein kinase-activated protein kinase-2 (MK-2).<br>References Anderson, D.R. et al.: J. Med. Chem., 50, 2647 (2007); Montagnoli, A. et al.: Nature Chem. Biol., 4, 357 (2008); Charych, D.H. et al.: J Cell. Biochem., 104, 1075 (2008); Jackson, P.K. et al.: Nature Chem. Biol., 4, 331 (2008);<br></p>

<p>Applications Semi-synrhetic antitumor agent derived from Illudin S. Inhibits DNA synthesis and induces apoptosis in tumor cells. Antineoplastic.<br>References Woynarowski, J.M., et al.: Biochem. Pharmacol., 54, 1181 (1997), Alexandre, J., et al.: Clin. Cancer Res., 10, 3377 (2004), Senzer, N., et al.: Am. J. Clin. Oncol., 28, 36 (2005),<br></p>