Apoptosis

<p>UK-101 is a potent and selective inhibitor of the immunoproteasome LMP2, inhibiting β1i (LMP2), β1c (LMP2), and β5 (LMP2), with IC50s of 104 nM, 15 μM, and 1 μM</p>

<p>UCB-5307 inhibits TNFR1, binds TNFα with 9 nM KD, shows slow kinetics (KD=6 nM), and penetrates hTNF/hTNFR1 complexes.</p>

<p>Erastin2 is an iron death inducer that induces cell death by binding to the lipophilic free radical trapping antioxidant ferrostatin-1 or the iron chelator DFO.</p>

<p>Antifolate C2 (AGF 154) inhibits tumor growth with 0.14 nM IC, useful in cancer/autoimmune research.</p>

<p>DB1976: Selenophene DB270 analog, inhibits PU.1 (IC50=10 nM), disrupts PU.1/DNA (KD=12 nM), induces apoptosis, cell-permeable.</p>

<p>MBM-55 is an effective inhibitor of NIMA related kinase 2 (NEK2) with an IC50 of 1 nM.</p>

<p>EGFR-IN-11 selectively blocks EGFR-tyrosine kinase and promotes apoptosis; targets EGFRL858R/T790M/C797S, IC50=18 nM; halts cell cycle at G0/G1.</p>

Ro 90-7501, an amyloid β42 (Aβ42) protofibril and TPR-dependent PP5 inhibitor, is a novel cervical cancer cell radiosensitizer that inhibits HCMV.

<p>Potent, oral Tubulin inhibitor 11 hinders polymerization, targets Colchicine site, induces mitotic block, and apoptosis.</p>

<p>HTH-01-091 is a potent and selective maternal embryonic leucine zipper kinase (MELK) inhibitor (IC50: 10.5 nM).HTH-01-091 inhibits PIM1/2/3, RIPK2, DYRK3,</p>

<p>EB1 is an MNK kinase inhibitor that inhibits cancer cell growth, promotes apoptosis, and inhibits eIF4E phosphorylation.</p>

<p>Imipramine (Dimipressin) is a Fascin1 inhibitor with antitumor activity and induces apoptosis.</p>

<p>Tiomolibdate diammonium (NSC-286644) blocks SOD1 and COX, acting as an antiangiogenic and antitumor agent.</p>

<p>RIPK3-IN-1 is a RIPK3 inhibitor (IC50: 9.1 nM) that inhibits c-Met kinase, RIPK1, and RIPK2 activity and can be used to study apoptosis.</p>

CMLD-2 is a HuR-ARE inhibitor (Ki: 350 nM) that promotes apoptosis, has antitumor properties, and reduces thyroid cancer cell viability.

<p>Alethine is a small antitumor compound used to treat cancers and infections, boosting T-cell cytotoxicity by raising TNFα.</p>

<p>BCP-T.A is an iron death inducer that acts by binding to GPX4.</p>

Epristeride (ONO-9302) is a steroidal 5-alpha-reductase isoform 2 inhibitor that inhibits SR isoform 2. Epristeride reduces prostate size.

<p>Ciglitazone: potent PPARγ agonist, EC50 3 μM, oral hypoglycemic; reduces insulin, blood pressure, Th17 cells, VEGF; halts gastric cancer growth.</p>

<p>Necrostatin-5 (Nec-5) inhibits RIP1 kinase, prevents cell necrosis, and protects Fadd-deficient Jurkat cells with an EC50 of 240 nM.</p>

<p>Mepazine, a MALT1 inhibitor, blocks GSTMALT1 (IC50: 0.83μM) and GSTMALT1 325-760 (IC50: 0.42μM), promoting apoptosis and reducing cell viability.</p>

<p>P505-15 Acetate inhibits spleen tyrosine kinase, reduces immune response and inflammation, and lowers arthritis severity.</p>

<p>HBDDE inhibits PKCα/γ (IC50: 43/50 μM), favors them over PKCδ/βI/βII, and induces neuronal apoptosis. Derived from ellagic acid.</p>

<p>Triparanol (NSC-65345) interferes with posttranslational modification of Hedgehog signaling molecules as well as the sterol sensing domain of its receptor PTCH1</p>

<p>Atrosab is a humanized IgG1 antibody targeting TNFR1, inhibiting TNF-mediated apoptosis, and can be used to study inflammatory and neurodegenerative diseases.</p>

<p>eIF4A3-IN-1 is an inhibitor of eukaryotic initiation factor 4A3 (eIF4A3). eIF4A3-IN-1 inhibits cytosolic nonsense-mediated RNA decay at high concentrations.</p>

<p>CSN5i-3 is a potent, selective, and orally available inhibitor of the proteolytic subunit of the CSN complex, CSN5, as an anticancer agent.Cost-effective and quality-assured.</p>

Minodronic acid (YM-529) is a P2X2/3 antagonist with anticancer properties, inhibiting cell growth and metastasis, and used in osteoporosis research.

<p>CTA 056 is an ITK inhibitor that inhibits the growth of MOLT-4 xenograft tumors in mice and can be used to study autoimmune disorders.</p>

<p>TT01001, a mitoNEET agonist, may treat type II diabetes by reducing oxidative stress and preventing neuronal death.</p>

<p>SPD304 dihydrochloride is a selective inhibitor of TNF-α with an IC50 of 22 µM. SPD304 dihydrochloride promotes dissociation of TNF trimers.</p>

<p>SYM 2081: Kainate receptor agonist, IC50 of 35 nM, depolarizes muscle, lowers EPSP amplitude.</p>

Gallium maltolate is a ribonucleoside-diphosphate reductase inhibitor.

HS38: DAPK-specific ATP-competitive inhibitor; Kds: DAPK1 (300 nM), PIM3 (200 nM), ZIPK (280 nM); useful in smooth muscle disorder research.

Triciribine phosphate (VD 002) is an AKT inhibitor that inhibits neovascularization and can be used in the study of leukemia.

Perphenazine dihydrochloride: Oral dopamine, histamine-1 antagonist; targets D2, D3, 5-HT2A, Alpha-1A; may treat psychiatric disorders, cancer.

OR-1896 is a PDE III inhibitor, a vasodilator with partial anti-inflammatory properties, and can be used to study heart failure and vascular dysfunction.

<p>CBS9106 (SL-801) is a CRM1 inhibitor with CRM1-degrading and anti-tumor activity that inhibits CRM1-dependent nuclear export.</p>

<p>GCN2-IN-1 (A-92) is an effective GCN2 inhibitor and can be used in research on the treatment of cancer as a chemotherapeutic agent.</p>

<p>A09-003 Inhibits the proliferation of leukemia cell lines and inhibits the increase of leukemia sequence-1 protein in HI bone marrow cells.</p>

AOH1160 is an inhibitor of proliferating cell nuclear antigen (PCNA).

ZDLD20 is a CDK4 inhibitor with anti-HCT116 and anticancer activity that inhibits colony formation and blocks the G1 phase of the cell cycle.

PARP/PI3K-IN-1 is a PARP and PI3K dual inhibitor with anticancer and antiproliferative activities for the study of breast, pancreatic and lung cancers.

<p>MJN68390 has an apparent IC50 value of 15 μM against CASP8 and shows no activity against CASP10.</p>

<p>FA16 is a selective, metabolically stable ferroptosis inducer with an IC50 value of 1.26 μM.FA16 is a derivative of 2-(trifluoromethyl)benzimidazole.FA16</p>

<p>N6-Cyclopentyladenosine (CPA) is a selective agonist of the adenosine A1 receptor and can be used to mimic the action of the adenosine A1 receptor, with Ki's of</p>

<p>JY-2 is a forkhead transcription factor O1 (FoxO1) inhibitor with antidiabetic activity that inhibits FoxO1 transcription and can be used to study psoriasis.</p>

<p>BCL6-IN-7 (BCL6 inhibitor-7) is a BCL6 corepressor-interaction inhibitor with potential antitumor activity, used in lymphoma research.</p>

HBED (CHELII) is an iron chelator and can be used in research on the treatment of chronic iron overload and acute iron poisoning.

<p>RET-IN-23 is an orally available and highly potent RET inhibitor with significant antitumor activity for the study of non-small cell lung cancer.</p>

Prinomastat: orally active, crosses blood-brain barrier, inhibits MMP-1/2/3/9, Ki/IC50s: 0.05-0.3/5.0-79 nM, antitumor.

<p>NSC49652 triggers apoptotic cell death dependent on p75NTR and JNK activity in neurons and melanoma cells, and inhibits tumor growth in a melanoma mouse model.</p>

<p>Ezatiostat HCl (TLK199) inhibits glutathione S-transferase, GSTP1-1 specifically, and may treat cytopenias.</p>

<p>DX3-235 is an oxidative phosphorylation (OXPHOS) inhibitor on mitochondrial complex I function in galactose-containing media, resulting in reduced ATP.</p>

<p>BIX selectively induces BiP/GRP78 and ER chaperone, preventing cell death in neurons and retinas.</p>

<p>EAD1 HCL is a potent autophagy inhibitor with antiproliferative activity in lung and pancreatic cancer cells. EAD1 HCL also induces apoptosis</p>

<p>Ethylene dimethanesulfonate has selective pro-apoptotic effects on LCs. Ethylene dimethanesulfonate is a mild alkylating, non-volatile methanesulfonic diester</p>

<p>MTI-31 (LXI-15029) is a potent oral mTORC1/2 inhibitor with a Kd of 0.20 nM, &gt;5,000-fold selectivity, and an IC50 of 39 nM.</p>

<p>Necrocide 1 is a inducer of cancer cell necrosis that is not inhibited by caspase, BCL2 , or TNFα, and acts through the mitochondrial regulatory pathway.</p>

<p>PRMT6-IN-3 is a selective PRMT6 inhibitor with an IC50 value of 192 nM.PRMT6-IN-3 has anticancer activity and induces apoptosis in cancer cells.</p>

<p>AAPK-25, a dual Aurora/PLK inhibitor, disrupts mitosis, induces apoptosis, and has antitumor properties.</p>

<p>Ferroptocide is a thioredoxin inhibitor that induces iron death in cancer cells and can be used in breast cancer research.</p>

MS-177 is a PROTAC EZH2 degrader that promotes cholangiocarcinoma growth through the EZH2-mediated WNT7B/β-catenin pathway.

"DC_AC50 inhibits Atox1/CCS to reduce cancer cell growth and prevent chemotherapy resistance."

<p>PDK4-IN-1 hydrochloride is an anthraquinone derivative and a potent and orally active inhibitor of pyruvate dehydrogenase kinase 4 (PDK4, IC50 value = 84 nM).</p>

<p>NSC 689534 forms a chelate with copper (Cu 2+), resulting in the NSC 689534/Cu 2+ complex, which is a potent inducer of oxidative stress and exhibits antitumor activity [1].</p>

<p>TC ASK 10 is a potent, selective and orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1,IC50 = 14 nM). The IC50 value for ASK2 is 0.51 μM.</p>

<p>GNE-900 is an ATP-competitive ChK1 inhibitor with selective and oral activity.GNE-900 inhibits ChKl and ChK2 with IC50 values of 0.0011 and 1.5 µM, respectively</p>

<p>NSC194598 is a p53 DNA-binding inhibitor, demonstrating an in vitro IC50 of 180 nM and an in vivo range of 2-40 μM.</p>

<p>Ogremorphin (GPR68-IN-1) is a potent inhibitor of GPR68, exhibiting an EC50 of 170 nM.it is utilized in the study of autoimmune chronic inflammatory diseases [1</p>

<p>Antitumor agent-60 inhibits growth by targeting RAS-RAF, binding CRAF (Kd: 721.3 nM), boosting p53/ROS, causing apoptosis, and arresting G2/M phase.</p>

<p>MK-2206 free base is an allosteric Akt inhibitor that is both potent and selective, administered orally, exhibiting IC50 values of 8, 12, and 65 nM for Akt1,</p>

<p>Lacutoclax (LP-108) is an orally active and selective Bcl-2 inhibitor with antitumor activity both in vivo and ex vivo，lymphoma and leukemia.</p>

<p>ICL-CCIC-0019 inhibits ChoKα, causes G1 arrest, ER stress, and cancer cell apoptosis.</p>

<p>HS148 selectively inhibits DAPK3 (Ki 119 nM), reducing gastric cancer progression via ULK1-dependent autophagy and tumor suppression pathways.</p>

<p>N-Oleoyl serinol, a ceramide analog, plays a crucial role in stem cell therapy by inhibiting the development of teratomas in stem cells. It triggers apoptosis in remaining pluripotent embryoid body-derived cells (EBCs), thwarts teratoma formation, and promotes the enrichment of EBC cells that proceed to neural differentiation post-transplantation [1].</p>

<p>(S)-Sabutoclax ((S)-BI-97C1), an optically pure derivative of apogossypol, serves as a pan-active inhibitor of the antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins. It effectively blocks the binding of BH3 peptides to key proteins in the family, including Bcl-XL, Bcl-2, Mcl-1, and Bfl-1, displaying inhibitory concentration (IC50) values of 0.31, 0.32, 0.20, and 0.62 μM, respectively. Furthermore, (S)-Sabutoclax demonstrates potent efficacy in inhibiting the growth of various cancer cell lines, such as those from human prostate cancer, lung cancer, and lymphoma, with half-maximal effective concentration (EC50) values of 0.13, 0.56, and 0.049 μM, respectively. This compound is utilized in research focusing on apoptosis-based cancer therapies [1].</p>

<p>Ethylene glycol dimethacrylate, a methacrylate monomer, demonstrates cytotoxic and genotoxic impacts on human gingival fibroblasts (HGFs), elevating</p>

<p>Lactoferrin 17-41 (Lactoferricin B) acetate, a peptide derived from bovine lactoferrin spanning residues 17-41, exhibits broad-spectrum antimicrobial properties against Gram-positive and Gram-negative bacteria, viruses, protozoa, and fungi. Additionally, this compound demonstrates antitumor activities [1] [2].</p>

<p>GCN2-IN-6: Potent, oral GCN2/PERK inhibitor; IC50s - GCN2: 1.8 nM (enzymatic), 9.3 nM (cellular); PERK: 0.26 nM (enzymatic), 230 nM (cellular).</p>

<p>YM281 is a potent EZH2 inhibitor, causes apoptosis and G0/G1 arrest, has antitumor activity in vivo, and may be researched for lymphoma.</p>

<p>BAI1 hydrochloride is a selective inhibitor of the apoptosis factor BAX, functioning through an allosteric mechanism. By binding to BAX, it allosterically inhibits its activation, showcasing potential applications in the research of diseases mediated by BAX-dependent cell death [1].</p>

<p>PLK1/BRD4-IN-1 (9b) is an orally active dual inhibitor of PLK1 (IC50: 22 nM) and BRD4 (IC50: 109 nM).</p>

<p>SM-433: Smac mimetic, blocks IAPs, strong XIAP BIR3 affinity (IC50 &lt;1 μM). See patent WO2008128171A2.</p>

<p>15-Deoxy-Δ12,14-Prostaglandin A1, a deoxyanalog of prostaglandins, inhibits NF-κB signaling and induces apoptosis. It also prevents TNF-α-induced upregulation of inflammatory endothelial cell adhesion molecules (CAM) and reduces monocyte arrest [1].</p>

<p>RET-IN-25 (compound 6b) is an anticancer RET kinase inhibitor that demonstrates efficacy against medullary thyroid carcinoma (MTC), exhibiting half-maximal</p>

(S)-Verapamil hydrochloride is an inhibitor of leukotriene C4 (LTC4) and calcein transport by MRP1,and leads to the death of potentially resistant tumor cells.

<p>CR-1-31-B, a synthetic rocaglate, inhibits eIF4A, hinders protein synthesis initiation, and induces apoptosis in cancer cells.</p>

<p>CNDAC, a nucleoside analog, is a major metabolite of oral drug sapacitabine.</p>

<p>Topoisomerase II inhibitor 15 (compound 2g) serves as a potent apoptotic inducer, exhibiting heightened selectivity for head and neck tumors [1].</p>

<p>Tylvalosin (Acetylisovaleryltylosin) is a broad-spectrum macrolide antibiotic with antibacterial and antiviral properties, effective against PRRSV infection.</p>

<p>NSC 48160 is an anti-pancreatic cancersmall molecule that inhibits growth and enhance apoptosis of pancreatic cancer cells through the mitochondrial pathway.</p>

<p>FGFR-IN-8, potent oral FGFR inhibitor for wild-type/mutant types, induces apoptosis with anti-cancer properties.</p>

<p>KRIBB3: novel anticancer microtubule inhibitor; halts MDA-MB-231 cell migration/invasion by targeting Hsp27 phosphorylation.</p>

<p>Nalmefene (ORF 11676) is a μ-opioid antagonist and partial κ agonist used to study opioid overdose and alcohol dependence.</p>

<p>RET-IN-17 inhibits RET kinase; may help in IBS pain and RET-activated cancers.</p>

<p>HJC0152 (free base) is an orally active, potent STAT3 inhibitor that impedes cell cycle progression, induces apoptosis, and notably reduces MDA-MB-231 xenograft</p>

<p>MAO-B-IN-26 (Compound IC9) serves as both a MAO-B and acetylcholinesterase inhibitor.</p>

<p>GDC-2394: Oral, selective NLRP3 inhibitor; blocks IL-1β (human 0.4μM, mouse 0.1μM), spares NLRC4.</p>

<p>TM5441, an orally bioavailable plasminogen activator inhibitor-1 (PAI-1) inhibitor with IC50 values ranging from 13.9 to 51.1 μM, effectively induces intrinsic apoptosis across multiple human cancer cell lines. Additionally, it mitigates Nω-nitro-l-arginine methyl ester-induced cardiac hypertension and vascular senescence [1] [2].</p>