Apoptosis

<p>Applications Intermediate in the production of cell death regulators and apoptosis promoters.<br>References Park, C., et al.: J. Med. Chem., 51, 6902 (2008),<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>Dibenz[a,h]anthracene (CCRIS 208) has induced DNA damage and gene mutations in bacteria and gene mutations and transformation in several types of mammalian cell</p>

<p>MI-773 (SAR405838 (MI 773)) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1.</p>

<p>Flurochloridone (R 40244) is a selective herbicide. Flurochloridone induces apoptosis and is regulated by mitochondrial dysfunction and oxidative stresses.</p>

<p>Riviciclib hydrochloride (P276-00) is a novel CDK1, CDK4 and CDK9 inhibitor with IC50 of 79 nM, 63 nM and 20 nM, respectively. Phase 2/3.</p>

<p>SU11274 (Met Kinase Inhibitor)(IC50=10 nM) is a specific Met inhibitor. It shows no significant effects on PGDFRβ, EGFR or Tie2.</p>

<p>NPB (Alpha-NPB) is a potent BAD phosphorylation inhibitor(at Ser99,IC50 of 0.41 μM.)</p>

<p>Camptothecin (CPT) belongs to the alkaloid group of natural products and is a specific DNA topoisomerase I (Topo I) inhibitor (IC50=679 nM) with specificity.</p>

<p>Cot inhibitor-2: Potent, selective Tpl2/MAP3K8 blocker. IC50: 1.6 nM; hampers LPS-induced TNF-α, IC50: 0.3 μM. Orally active.</p>

<p>L-Cystathionine: nonprotein amino acid; important for sulfur amino acid metabolism; used in cardiovascular research.</p>

<p>GEA 3162 blocks ADP-induced platelet clumping in PRP and boosts cGMP in granulocytes and leukocytes.</p>

<p>Rhosin is a specific inhibitor of RhoA GTPases (Kd: ~0.4 uM), blocking RhoA-GEF interaction, not affecting Cdc42/Rac1/LARG, and induces apoptosis.</p>

<p>(5Z,2E)-CU-3 is a potent and selective inhibitor of DGKα isozyme with an IC50 value of 0.6 μM and inhibition of DGKα by competing ATP with a Km value of 0.48 mM</p>

<p>RET-IN-22 (compound 17b) is a potent, selective, and orally active inhibitor of RET, exhibiting IC50 values of 20.9 nM for wild-type RET and 18.3 nM for RET-</p>

<p>CMLD010509 (SDS-1-021) inhibits oncogenic proteins MDM2, CCND1, MYC, MAF, MCL-1 in multiple myeloma.</p>

<p>Nampt-IN-3 simultaneously inhibit nicotinamide phosphoribosyltransferase (NAMPT) and HDAC (IC50s of 31 nM and 55 nM, respectively).</p>

<p>MMP-9-IN-4 inhibits MMP-9 (IC50=7.46nM) and AKT (IC50=8.82nM), induces apoptosis and is used in cancer research.</p>

<p>Tezacitabine, a nucleoside analogue, inhibits ribonucleotide reductase, disrupts DNA replication, and induces apoptosis in tumor cells.</p>

<p>PDE5/HDAC-IN-1 is a potent inhibitor of phosphodiesterase 5 (PDE5) and HDAC, with IC50 values of 46.3 nM and 14.5 nM, respectively.</p>

<p>Antitumor agent-44 (Compound 5n) elicits potent antitumor effects by inducing disruption of mitochondrial homeostasis, cell cycle arrest, and apoptosis in human</p>

<p>BR102375 is a non-TZD PPAR γ full agonist (EC50: 0.28 μM) for the treatment of type 2 diabetes.</p>

<p>LLL3 is a small molecule STAT3 inhibitor.</p>

<p>BRD4 Inhibitor-15 targets BRD4 with 18 nM IC50, induces apoptosis in 22RV1 cells, and lowers c-Myc, aiding prostate cancer research.</p>

<p>AP1867 is a synthetic FKBP12F36V-directed ligand.</p>

<p>RIPK1-IN-15 (Compound 2.5) is a potent RIPK1 inhibitor that has the potential in neurodegenerative, autoimmune, and inflammatory diseases research [1].</p>

<p>HJC0416 is a potent orally bioavailable signal transducer and activator of transcription 3 inhibitor.</p>

<p>Vin-C01, a potent protector of pancreatic β-cells (EC50=0.22μM), aids in type 2 diabetes research by preventing STZ-induced β-cell apoptosis.</p>

<p>Famitinib (SHR1020), an oral drug, inhibits c-kit, VEGFR-2, and PDGFRβ (IC50: 2.3/4.7/6.6 nM) and triggers apoptosis in gastric cancer.</p>

<p>Oxythiamine chloride is a thiamine antagonist and anticancer agent that inhibits transketolase, affecting RNA/DNA synthesis and inducing apoptosis.</p>

<p>ZML-8 selectively inhibits Top1, blocks G2/M phase, causes DNA damage, and induces apoptosis with anti-tumor properties.</p>

<p>Atopaxar (E5555), a reversible PAR-1 thrombin receptor antagonist, interferes with platelet signaling.</p>

<p>CAY10506, a hybrid lipoic acid-TZD, activates PPARγ to control glucose and lipid levels with an EC50 of 10 μM.</p>

<p>RIP1 Kinase Inhibitor 6 is a potent and selective inhibitor of RIP1 kinase, demonstrating inhibitory activity with an IC50 of less than 100 nM in a human R1P1</p>

<p>Tubulin/HDAC-IN-1 is a dual inhibitor for tubulin &amp; HDAC8, blocking polymerization &amp; targeting HDAC8 (IC50: 150 nM), and induces cancer cell apoptosis.</p>

<p>Pentabromophenol (NSC-5717) suppressed TGF-β response by accelerating the turnover rate of TGF-β receptors.</p>

<p>(E)-[6]-Dehydroparadol ((6)-Dehydroparadol), an oxidative metabolite of [6]-Shogaol, is a potent Nrf2 activator.</p>

<p>W146 TFA is a selective sphingosine-1-phosphate receptor 1 ( S1PR1 ) antagonist with an EC 50 value of 398 nM.</p>

<p>TH1834 dihydrochloride is a specific Tip60 histone acetyltransferase inhibitor.</p>

<p>ML132 is an effective and selective inhibitor of caspase 1 (IC50: 0.316 nM).</p>

<p>HL271, a derivative of metformin, is a potent AMPK activator that increases AMPK phosphorylation. HL271 attenuates aging-associated cognitive impairment.</p>

<p>Topoisomerase IIα-IN-3 is a DNA-inserting topoisomerase-Iiα inhibitor that blocks the cell cycle in G0/G1 phase and induces apoptosis.</p>

<p>EGFR-IN-56 (13a) inhibits EGFR, EGFRT790M (IC50: 541.7nM), EGFRT790M/L858R (IC50: 132.1nM), blocks G2/M phase, and triggers apoptosis.</p>

<p>HS-438 inhibits imatinib-resistant BCR-ABL T315I mutation in chronic myeloid leukemia.</p>

<p>EAPB 02303, a microtubule inhibitor, induces mitotic arrest, spindle impairment, apoptosis, and has antitumor effects, enhancing Paclitaxel.</p>

<p>Ro 31-7837 is an opener of potassium channel.</p>

<p>Atopaxar, a reversible PAR-1 thrombin receptor antagonist, interferes with platelet signaling.</p>

<p>2,5-Dihydroxybiphenyl: a small molecule that induces trichothiodystrophy A protein dimerization, modulating TFIIH activity.</p>

<p>Compound 14d inhibits HDAC1 (IC50=70.7μM), HDAC2 (23.1μM), CDK2 (0.80μM), blocks cell cycle, induces apoptosis, and shows in vivo anti-tumor effects.</p>

<p>Nutlin-1 is a p53-MDM2 binding inhibitor, p-Glycoprotein (p-gp) transport substrate, and antitumor agent.</p>

<p>Apoptosis inducer 10 is a potent apoptosis inducer with anti-proliferative activity.</p>

<p>DRI-C21041 is a potent inhibitor of the CD40/CD40L interaction, demonstrating an inhibitory concentration 50 (IC50) value of 0.31 μM.</p>

<p>RIPK3-IN-2 is a RIP3 inhibitor that can be used in studies of diseases caused by or associated with activated necrotic pathways.</p>

<p>Anticancer agent 77 exhibits anticancer effects and can be used extensively in synthetic and medicinal chemistry studies.</p>

<p>GW7845, an L-tyrosine derivative, is a PPAR-γ agonist.</p>

<p>TP-472 is a selective inhibitor of BRD9 (Kd: 33 nM).</p>

<p>eIF4A3-IN-2 is a highly selective and noncompetitive eukaryotic initiation factor 4A-3 inhibitor with an IC50 of 110 nM.</p>

<p>SMI-6860766 is a CD40-Traf6 interactions blocker that acts by ameliorating the complications of diet-induced obesity in mice.</p>

<p>Nimustine: treats brain tumors, used with other drugs or radiotherapy for neoplasms.</p>

<p>"Motixafortide blocks CXCR4 with 1 nM potency. BMS-1166 hinders PD-1/PD-L1, boosting T cell activation, IC50: 1.4 nM."</p>

<p>RETRA is an agent of anticancer that acts by exerting anticancer activity in Ewing's sarcoma cells independent of their TP53 status.</p>

<p>AKCI is a PPI inhibitor that acts by targeting the AURKC-IκBα interaction.</p>

<p>Compound 2g, an anticancer agent, disrupts cell cycle and induces apoptosis for cancer research.</p>

<p>Perillic acid, a perillyl alcohol metabolite, induces lung cancer cell arrest, apoptosis, and has anti-HSV-1 and immune-modulating effects.</p>

<p>Zonisamide sodium is a 1,2 benzisoxazole derivative. It is the first agent of this chemical class to be developed as an antiepileptic drug.</p>

<p>Antitumor agent-62 releases NO, inhibits cancer cell growth, triggers apoptosis, and halts cell cycle at G2/M.</p>

<p>Compound A13 inhibits PD-1/PD-L1, enhances interferon-γ, lacks toxicity, and boosts immune response in co-culture models. IC50=132.8 nM.</p>

<p>potassium channel blocker</p>

<p>Tubulin-IN-26 blocks microtubule formation at colchicine site; IC50 4.64μM; may help in lung cancer study.</p>

<p>GLUT4-IN-2, selective GLUT4 blocker; IC50: 6.8μM (GLUT4), 11.4μM (GLUT1). Induces apoptosis, G0/G1 arrest, has antitumor effects.</p>

<p>TNF-α-IN-18 is a small molecule TNF-α inhibitor that blocks NF-κB translocation, alleviates sepsis in models, and protects against rheumatoid arthritis in mice.</p>

<p>LG190178, a vitamin D receptor (VDR) ligand, is a therapeutic agent used for the treatment of psoriasis, osteoporosis, and secondary hyperparathyroidism.</p>

<p>Compound 8a is an apoptotic agent that boosts Fas receptor and Cyto C genes to fight cancer with low toxicity.</p>

<p>VEGFR-2/BRAF-IN-1 inhibits VEGFR-2, BRAF V600E &amp; BRAF WT with IC50 of 49, 63 and 5 nM, triggers apoptosis, and halts G1/S cell cycle.</p>

<p>GZD856 is an orally bioavailable PDGFRα/β inhibitor (IC50s: 68.6 and 136.6 nM) with anti-lung cancer activities.</p>

<p>ASK1-IN-3, selective ASK1 inhibitor with 33.8 nM IC50; inhibits cell cycle kinases; induces apoptosis in HepG2 cells.</p>

<p>Bozepinib is an antitumor compound that acts by inducing PKR-mediated apoptosis and synergizing with IFN.</p>

<p>c-Met-IN-9 is a 4-phenoxypyridine derivative and a c-Met kinase inhibitor (IC50: 12 nM). c-Met-IN-9 induces apoptosis and shows antitumour effects.</p>

<p>TL02-59 dihydrochloride is an orally active inhibitor of Src-family kinase Fgr (IC50: 0.03 nM).</p>

<p>BP-1-108 is a potent and selective STAT5 inhibitor.</p>

<p>WJ35435 is a histone deacetylase and topoisomerase I dual inhibitor.</p>

<p>RXR agonist</p>

<p>BLM-IN-1: BLM inhibitor, KD 1.81 μM, IC50 0.95 μM; causes DNA damage, apoptosis, stops cancer cell growth.</p>

<p>UCD38B HCl, a cell-permeable uPA inhibitor, induces programmed necrosis in high-grade glioma cells.</p>

<p>Anti-melanoma agent 1 (Compound 5m) is an anti-melanoma agent that induces apoptosis.</p>

<p>RET-IN-20: potent RET inhibitor (IC50 = 13.7 nM), reduces p-Ret/p-Shc, induces apoptosis, anti-tumor effects.</p>

<p>Topoisomerase I (Compound ZML-14) inhibitor 3 induces HepG2 cell apoptosis and arrests cell cycle at G2/M phase.</p>

<p>Quinidine Monosulfate: an oral antiarrhythmic, CYP450db inhibitor, K+ blocker (IC50 19.9 μM), used in malaria research.</p>

<p>Anticancer agent 67 is a ciprofloxacin analogue, an anticancer agent that induces apoptosis and increases sub-G1 cell populations in MCF-7 cells.</p>

<p>EGFR-IN-52, a potent EGFR inhibitor, has IC50s: 0.358 μM (wild-type), 86.02 μM (L858R-TK), 432.67 μM (T790M-TK); induces cancer cell apoptosis.</p>

<p>"SPRC, a synthetic antioxidant, boosts H2S production, activates STAT3, and guards against doxorubicin heart damage."</p>

<p>CAY10789: potent CysLT1R antagonist (IC50 2.8 µM), GPBAR1 agonist (EC50 3 µM), reduces U937 cell adhesion, TNF-α, stable with promising pharmacokinetics.</p>

<p>P2Y6 receptor agonist</p>

<p>MMP-9-IN-5: MMP-9 and AKT inhibitor (IC50: 4.49 nM and 1.34 nM), induces apoptosis for cancer research.</p>

<p>CDK9-IN-18: Potent CDK9 blocker, anticancer, induces apoptosis, low cellular activity.</p>

<p>Compound 4j: potent anticancer agent; halts cell growth, induces apoptosis and G0/G1 arrest; significant in vivo tumor reduction.</p>

Antiproliferative agent-19 induces apoptosis and G2/M cell cycle arrest in lung cancer cells.

<p>TPB15, an oral Hh inhibitor, blocks Smo activity, arrests cell cycle, induces apoptosis, and shows potent antitumor effects with low toxicity.</p>