Apoptosis

<p>AEG 3482 blocks JNK, induces HSP70, binds HSP90, and boosts HSP25 expression, preventing cell death.</p>

<p>AZD5582 TFA is a potent IAP antagonist that binds to the BIR3 domain of cIAP1, cIAP2, and XIAP with IC50 values of 15, 21, and 15 nM, respectively.AZD5582 TFA</p>

<p>VPC-70063 (Thiourea, N-[3,5-bis(trifluoromethyl)phenyl]-N'-(phenylmethyl)-) is an inhibitor of c-Myc-MAX.</p>

<p>A unique collection of 193 endoplasmic reticulum stress (ER stress) related compounds used for high throughput screening (HTS) and high content screening (HCS);</p>

<p>CWI1-2 is a potent IGF2BP2 inhibitor that inhibits its interaction with M6A-modified target transcripts by binding IGF2BP2.</p>

<p>Necroptosis-IN-3 (Cyclohexanecarboxamide, N-(2-thienylmethyl)-) (Compound 69) is a Necroptosis inhibitor that inhibits TNF-α induced necroptosis.</p>

<p>iNOs-IN-5 (Compound BN-4) is an inhibitor of iNOS with an IC50 value of 0.1707 μM, effectively reducing NO expression in RAW264.7 cells stimulated by LPS (HT-D1056). It further diminishes the expression of ROS and lactate dehydrogenase induced by hypoxic injury, displaying anti-necrotic and anti-apoptotic properties. In an SD rat model, iNOs-IN-5 exhibits neuroprotective effects against cerebral ischemia and is capable of crossing the blood-brain barrier.</p>

<p>hCAIX-IN-23 (Compound 27) is a human carbonic anhydrase (hCA) inhibitor with Ki values of 10.4 nM for hCA IX and 8.5 nM for hCA XII. It not only inhibits hCA activity but also releases NO, exerting dual anti-tumor effects. By reducing the expression of hCA IX and iron regulatory proteins, hCAIX-IN-23 regulates mitochondrial caspase activity and the ferroptosis pathway, thereby inducing apoptosis. This compound is utilized in research focused on renal cancer.</p>

<p>CDK-IN-14 (B34) is a CDK2 inhibitor (IC50=0.097 μM) that exhibits anti-hepatocellular carcinoma activity. It inhibits the cell cycle in HepG-2 cancer cells and induces apoptosis (apoptosis) through a caspase-mediated mechanism.</p>

<p>CDK/HDAC-IN-4 is a highly selective dual inhibitor of cyclin-dependent kinase (CDK) and histone deacetylase (HDAC), with IC50 values of 88.4 nM and 168.9 nM, respectively. This compound exhibits antiproliferative effects in both hematologic and solid tumor cells. Additionally, CDK/HDAC-IN-4 induces apoptosis and S-phase cell cycle arrest in MV-4-11 cells. It has also demonstrated significant antitumor efficacy in an MV-4-11 xenograft model.</p>

<p>1,2,3,4-Tetrahydronaphthalen-2-ol exhibits weak inhibitory activity against Bcl-xL and is widely used in biochemical experiments and drug synthesis research.</p>

<p>RIPK1-IN-17 is a dual inhibitor of RIPK1 and RIPK3 inhibits necrosis by inhibiting phosphorylation of RIPK1, RIPK3 and MLKL,in a tnf-induced inflammation model.</p>

<p>Tubulin/AKT1-IN-1 (Compound D1-1) serves as an inhibitor of both tubulin polymerization and AKT pathway activation, effectively suppressing proliferation and</p>

<p>Compound 24a, an FPR1 antagonist, demonstrates potent inhibition of the formyl peptide receptor 1 (FPR1) with an IC50 value of 25 nM.</p>

<p>Trichostatin C, a natural glycosylated hydroxamate, is a histone deacetylase inhibitor with antifungal properties and can induce cell differentiation.</p>

<p>RSM3 TFA is a stapled peptide and an inhibitor of METTL3-METTL14, exhibiting a dissociation constant (Kd) of 3.10 μM. It inhibits tumor growth and induces cell apoptosis. RSM3 TFA is utilized in cancer research.</p>

<p>Anticanceragent 272 (Compound 2) is an anticancer agent demonstrating significant activity against bladder cancer cells (T-24) with an IC50 of 2.81 μM. It depletes glutathione (GSH) through a Fenton-like reaction, generating reactive oxygen species (ROS) and hydroxyl radicals (•OH), thereby inducing apoptosis and ferroptosis. Anticanceragent 272 enhances chemodynamic therapy (CDT) and promotes tumor cell death through mitochondrial dysfunction and autophagy. It holds potential for further research in bladder cancer.</p>

<p>Pipernonaline is a useful organic compound for research related to life sciences. The catalog number is T124000 and the CAS number is 88660-10-0.</p>

<p>eIF4E-IN-2 effectively inhibits eIF4e, crucial for research on diseases like cancer.</p>

<p>DB2115 (tertahydrochloride) inhibits PU.1, key in leukemia; potential for cancer research.</p>

<p>RO7567132 is a bispecific antibody that binds and agonizes LTBR bivalently while binds and antagonizes FAP monovalently, inducing the formation of local TLS.</p>

<p>Anti-Mouse PD-1 Antibody (D265A) is an IgG2a, κ antibody inhibitor derived from mice, specifically targeting mouse PD-1.</p>

Calphostin C is a protein kinase C inhibitor.

<p>Ac-LEHD-AMC, a fluorogenic caspase-9 substrate, releases fluorescent AMC upon cleavage, aiding caspase-9 activity measurement.</p>

<p>PKM2-IN-8 (Compound 9b) is an inhibitor of pyruvate kinase M2 (PKM2) with an IC50 of 0.31 μM. It exhibits potent antiproliferative activity against U87MG glioma cells. PKM2-IN-8 induces early apoptosis and reduces lactate levels. This compound is useful for research in glioblastoma.</p>

<p>DAPK Substrate Peptide is a synthetic peptide substrate for death-associated protein kinase (DAPK) (Km = 9 μM).</p>

<p>PROTAC AR Degrader-8 (Compound NP18) functions as a PROTAC degrader targeting the androgen receptor (AR) and effectively degrades AR-FL in both 22Rv1 and LNCaP cells with DC50 values of 0.018 μM and 0.14 μM, respectively. It also degrades AR-V7 in 22Rv1 cells with a DC50 of 0.026 μM. Additionally, PROTAC AR Degrader-8 inhibits the proliferation of 22Rv1 and LNCaP cancer cells, exhibiting IC50 values of 0.038 μM and 1.11 μM. It induces cell cycle arrest at the G2/M phase and triggers apoptosis in 22Rv1 cells (apoptosis). Demonstrating anticancer efficacy, PROTAC AR Degrader-8 shows activity in both mouse and zebrafish models. [Pink: ligand for target protein AR ligand-33; Black: linker; Blue: ligand for E3 ligase Cereblon]</p>

<p>Gemcitabine monophosphate disodium salt is a monophosphate derivative of Gemcitabine.</p>

<p>Isoharringtonine, an alkaloid from Cephalotaxus koreana, inhibits and induces apoptosis in cancer cells.</p>

<p>(+)-Mcl-1 inhibitor 22 (Example 37) is an MCL-1 inhibitor that impedes the anti-apoptotic function of MCL-1 by blocking its interaction with pro-apoptotic proteins. It demonstrates antiproliferative activity against various cancer cell lines and is applicable for cancer research.</p>

Chaetoglobosin A, the active compound extracted of Penicillium aquamarinium, is a member of the cytochalasan family. It preferentially induces apoptosis.

<p>Waltonitone is a natural ursane-type pentacyclic triterpene isolated from Gentian waltonii Burkill.</p>

<p>Enniatin complex: fungal cyclohexadepsipeptides inhibit enzymes, induce cancer cell apoptosis, and have ionophoric, antibiotic, and hypolipidemic effects.</p>

<p>Ferroptosis-IN-13 (compound NY-26) is an inhibitor of ferroptosis. It effectively suppresses RSL3-induced ferroptosis in 786-O cells, with an EC50 value of 62 nM.</p>

<p>WAY-118959-A is a potential microtubule acetylation inhibitor.</p>

<p>Sorafenib D4 is deuterium-labeled Sorafenib, a multi-kinase inhibitor (Raf-1, B-Raf, VEGFR-3) with IC50s: 6, 20, 22 nM.</p>

<p>Neocarzinostatin is an effective DNA-damaging, anti-tumor antibiotic.</p>

MTX-23, an AR-targeted Proteolysis Targeting Chimera (PROTAC), effectively degrades both AR-V7 and AR-FL, inhibiting the proliferation of CaP cells and inducing

<p>Mangafodipir trisodium can enhance contrast in magnetic resonance imaging (MRI) of the liver, is a contrast agent delivered intravenously.</p>

<p>Tauro-β-muricholic acid (TβMCA), a trihydroxylated bile acid, acts as a competitive and reversible FXR antagonist (IC 50 = 40 μM) and exhibits antiapoptotic</p>

<p>8-Bromo-cAMP is a cell-permeable cAMP analogue and activator of CAMP-dependent protein kinase A that induces cell death and reduces proliferation.</p>

<p>EGFR/BRAFV600E-IN-4 (Compound 10f) is a dual inhibitor of EGFR and BRAFV600E, with IC50 values of 61 nM and 43 nM, respectively. It halts the cell cycle, induces apoptosis in both early and late stages, and inhibits cancer cell growth in vitro, showing broad-spectrum anticancer activity.</p>

<p>MYC-RIBOTAC, a ribonuclease-targeting chimera (RIBOTAC) specific to the MYC internal ribosome entry site (IRES), comprises an MYC mRNA-binding element tethered</p>

<p>EGFR-IN-86 (compound 4i), an EGFR inhibitor (IC50: 1.5 nM), demonstrates potent activity against glioblastoma by inducing apoptosis and causing G2/M phase cell</p>

<p>PROTAC Bcl-xL degrader-3 is a potent ROTAC Bcl-xL degrader.</p>

MD-222: a first-in-class, highly potent PROTAC that degrades MDM2, activates p53, and exhibits anticancer properties.

<p>LH1307 blocks PD-1/PD-L1 interaction, IC50 = 3 nM (HTRF assay), activates Jurkat cells, EC50s: 79 nM (U2OS), 763 nM (CHO).</p>

<p>FF2039 (compound 1j) is a PROTAC degrader specifically targeting HDAC1, HDAC6, and various subtypes of class I, IIa, and IIb HDACs. It induces cell cycle arrest and apoptosis, showing significant antiproliferative activity against both hematological and solid tumor cell lines. The IC50 values for FF2039 against HDAC1, HDAC2, HDAC4, and HDAC6 are 1.03, 2.15, 12.4, and 0.053 μM, respectively. FF2039 exhibits antiproliferative effects on solid tumors such as MM.1S, MDA-MB-231, and U-87MG, with EC50 values of 2.8, 28, and 30 μM, respectively.</p>

<p>Compound 13b, a potent EGFR degrader, inhibits and induces apoptosis in NSCLC cells with a DC50 of 13.2 nM.</p>

<p>8-Aminoadenosine reduces ATP, blocks mRNA synthesis, and Akt/mTOR signaling, triggering autophagy and apoptosis independently of p53, with antitumor effects.</p>

<p>S-Adenosyl-L-methionine (Ademetionine) is an intermediate metabolite of methionine,for treatment of primary biliary cirrhosis and major depressive disorder.</p>

<p>EGFR/HER2/DHFR-IN-3 (compound 4c) serves as an efficacious dual inhibitor specifically targeting EGFR/HER2, exhibiting IC50 values of 0.138 μM for EGFR and 0.</p>

<p>TNF/IFNγ-IN-1 (TGA) is a TNF and IFN-γ inhibitor with antioxidant and anti-inflammatory activities for neurodegenerative diseases such as Alzheimer.</p>

<p>HDAC6-IN-16 (compound 5c), a quinazolin-4(3H)-one-based inhibitor of histone deacetylase 6 (HDAC6), demonstrates an anticancer effect by inhibiting colony</p>

<p>SI-2, a SRC-3 inhibitor, triggers breast cancer cell death (IC50: 3-20 nM), sparing normal cells.</p>

<p>Thalidomide-based E3 ligase ligand linked to a PROTAC piperazine-piperidine chain.</p>

<p>β-Glucuronide-dPBD-PEG5-NH2 TFA is a β-glucuronide-linked pyrrolobenzodiazepine dimer employed in the synthesis of the antibody-drug conjugate (ADC) cIRCR201-</p>

<p>PROTAC Bcl-xL degrader-2, based on von Hippel-Lindau ligand, is a potent degrader of Bcl-xL (a Bcl-2 family member), demonstrating an IC 50 of 0.6 nM.</p>

Disitertide (P144) is an inhibitor of TGF-β1.

<p>YN14-H is a PROTAC degrader that targets KRASG12C. It effectively inhibits the growth of NCI-H358 and MIA PaCa-2 cells, with IC50 values of 0.042 μM and 0.021 μM, respectively, and DC50 values of 28.9 nM and 18.1 nM. YN14-H significantly induces apoptosis and suppresses cell migration. It demonstrates favorable pharmacokinetics and excellent in vivo antitumor activity.</p>

<p>Functionalized cereblon ligand with E3 ligase and alkylC5 linker for PROTAC R&amp;D; ready for protein conjugation. Formerly Pomalidomide-linker 4.</p>

<p>Thalidomide-O-C5-acid, a synthesized E3 ligase linker, merges cereblon and PROTAC tech.</p>

<p>EM 163是一种 TIR-TIR 相互作用抑制剂，它是MyD88蛋白的TIR（Toll/白细胞介素-1受体）结构域拟态。EM 163针对IL-1受体中的TIR 结构域，阻断与MyD88的相互作用。EM 163抑制葡萄球菌肠毒素B（SEB）引起的体内炎症细胞因子的产生。EM 163能保护小鼠免受SEB 冲击引起的死亡。在体外的大鼠海马神经元中，EM 163阻断p38的激活和IL-1β对化学诱导的长期电位（LTP）引发的蛋白质合成的抑制作用。</p>

<p>Taxamairin B is a potent anti-inflammatory compound that inhibits the expression of proinflammatory cytokines (TNF-α, IL-1β, and IL-6) and reduces the</p>

<p>SH-5, an AKT inhibitor potentiates apoptosis and inhibits invasion through the suppression of anti-apoptotic, proliferative and metastatic gene products</p>

<p>IPH10 is an anticancer agent with strong antitumor effects in vivo and exhibits no liver or kidney toxicity. It significantly increases the reactive oxygen species (ROS) levels in tumor cells, decreases mitochondrial membrane potential, and induces apoptosis (apoptosis) in these cells.</p>

<p>Betamethasone (NSC-39470), a glucocorticoid steroid, has immunosuppressive and anti-inflammatory properties.</p>

<p>KRASG12C IN-16 (Compound SK-17) is a selective, covalent, and orally active KRASG12C inhibitor. It can induce apoptosis and effectively prevent the activation of the MAPK and PI3K/mTOR signaling pathways. Additionally, KRASG12C IN-16 exhibits antitumor activity against pancreatic cancer.</p>

<p>AChE-IN-81 (compound 22) is a reversible, selective inhibitor of AChE with an 80.0% inhibition rate and an IC50 of 3.7 μM. It binds to AChE with an affinity (Kd) of 5.37 μM. AChE-IN-81 effectively reduces apoptosis in zebrafish brain cells and shows potential neuroprotective activity in an H2O2-induced SH-SY5Y cell damage model.</p>

<p>Anticanceragent 268 (Compound 4k) is a potential antitumor agent. It exhibits antiproliferative effects on HepG2 cells, with an IC50 value of 6.08 μM. Additionally, Anticanceragent 268 induces apoptosis and inhibits colony formation and migration of HepG2 cells.</p>

<p>Thalidomide-O-amide-C5-NH2 is a synthetic E3 ligase linker combining cereblon ligand and PROTAC linker.</p>

<p>NF-κB-IN-19 (Compound 8) is an NF-κB inhibitor. It effectively induces DNA damage in tumor cells through the NF-κB signaling pathway and promotes the production of reactive oxygen species (ROS), as well as induces autophagy and apoptosis. Additionally, NF-κB-IN-19 inhibits levels of VEGF and HIF-1α, exerting antiproliferative effects in tumor cells through the PI3K/AKT and STAT-3 pathways. It is also effective in overcoming cisplatin resistance and exhibits antitumor activity.</p>

<p>ROCK/HDAC-IN-2 (Compound C-9) is a dual inhibitor of ROCK/HDAC, characterized by IC50 values of 0.185 µM for HDAC6, 0.8 µM for ROCK1, and 0.7 µM for ROCK2. It effectively induces apoptosis and mitochondrial membrane potential alterations in cancer cells and demonstrates notable antitumor activity, making it useful for research in pancreatic ductal adenocarcinoma (PDAC) and triple-negative breast cancer (TNBC).</p>

PROTAC CARM1/IKZF3 degrader-1 (Compound 074) inhibits CARM1, reducing the methylation level of its substrate BAF155. This PROTAC degrader works by degrading IKZF 1/3 via a CRBN-dependent mechanism. It suppresses MYC protein expression, thereby inhibiting the proliferation of various multiple myeloma cells. Additionally, PROTAC CARM1/IKZF3 degrader-1 can induce apoptosis in H929 cells and overcomes resistance to immunomodulatory drugs (IMiDs, such as pomalidomide). It is applicable for cancer and immunology research. (Pink: ligand for target protein CARM1/IKZF3 ligand 1; Active form of target protein ligand: EZM 2302; Black: linker; Blue: ligand for E3 ligase Cereblon Thalidomide 4-fluoride)

<p>MC-25B is a selective FKBP12 PROTAC degrader. It effectively degrades FKBP12 with a DC50 of 0.35 μM and a Dmax of 89%. MC-25B facilitates the degradation of nuclear-localized FKBP12 through a mechanism dependent on DCAF16.</p>

<p>GL392 is a senolytic agent that delivers the potent senescence-clearing compound Dasatinib specifically to senescent cells. By targeting the LBD domain, it binds lipofuscin in these cells and releases Dasatinib via an ester linkage, inducing apoptosis (Apoptosis) in senescent cells. Additionally, GL392 is encapsulated in PEO-b-PCL microcapsules to ensure efficient intracellular delivery while minimizing systemic toxicity. GL392 is applicable in cancer research.</p>

<p>10-SLF is a PROTAC FKBP12 degrader. It facilitates the formation of a ternary complex between FKBP12 and FBXW7-R465C, leading to the proteasomal degradation of FKBP12 in a FBXW7-R465C-dependent manner. 10-SLF selectively reduces FKBP12 levels in cells that express FBXW7-R465C.</p>

C-Met/Axl-IN-1 (Compound 22a) is an oral, selective type II c-Met/Axl inhibitor with IC50 values of 1 nM and 10 nM, respectively. It effectively suppresses tumor cell proliferation, induces cell cycle arrest, and apoptosis (apoptosis), showcasing potent anti-tumor activity.

<p>ACBI3 is a pan-KRAS degrader with anticancer activity, degrading oncogenic KRAS.</p>

<p>Siomycin A: thiopeptide antibiotic, selectively inhibits FOXM1, anti-tumor, induces apoptosis.</p>

<p>Carubicin, an anthracycline antibiotic from Actinomadura carminata, disrupts DNA replication and repair by intercalating DNA and inhibiting topoisomerase II.</p>

<p>Fisetin quarterhydrate, a natural flavonol present in numerous fruits and vegetables, exhibits benefits including antioxidant, anticancer, and neuroprotective</p>

<p>BWA-522 is a small molecule, orally available protein-targeting chimera (PROTAC) that potentates the degradation of both full-length androgen receptor (AR-FL)</p>

<p>Estradiol cypionate (Depofemin), the 17 β-cyclopentylpropinate ester of estradiol, inhibits ET-1 synthesis via estrogen receptor.</p>

<p>dMCL1-2 is a PROTAC-based MCL1 degrader, binding at 30 nM, and induces apoptosis in leukemia.</p>

<p>ILS-920, a Rapamycin analog, has reduced immunosuppression, enhanced neuroprotection, and preferentially binds FKBP52 and L-type VGCC β1.</p>

<p>Apoptosis Inducer 3 (Compound 3), a selective apoptosis triggering agent, induces both apoptosis and late-apoptosis phases, demonstrating cytotoxic effects</p>

<p>FHD-286 is an inhibitor of BRM/BRG1 ATPase and can be used for studies on the treatment of BAF-related disorders such as acute myeloid leukemia.</p>

<p>Monactin is a Marcrotetrolide antibiotic produced by cycloheximide producing species of Streptomyces. It is a homolog of nonactin from the same species.</p>

<p>7-Methoxy-1-tetralone may have insecticidal activity.</p>

<p>Thalidomide-O-amido-PEG3-C2-NH2 is a cereblon ligand-linker for PROTACs with a 3-unit PEG.</p>

<p>HMGB1-IN-1 (compound 6) exhibits potent inhibition of NO production in RAW264.7 cells, with an IC50 of 15.9 ± 0.6 μM, and effectively disrupts the HMGB1/NF-κB/</p>

<p>PK095 is a proprietary compound in the guanidine - based F1F0-ATPase inhibitor family.</p>

<p>HDAC-IN-57 is an orally active pan-inhibitor of histone deacetylase (HDAC), inhibiting HDAC1, HDAC2, HDAC6, and HDAC8 with IC50 values of 2.07 nM, 4.71 nM, 2.4</p>

<p>Compound (Ra)-10, also known as Mcl-1 inhibitor 14, is a potent inhibitor of myeloid cell leukemia-1 (MCL-1), exhibiting a K_i of 0.018 nM, and holds potential</p>

<p>HC Toxin: cyclic tetrapeptide, reversible HDAC inhibitor (IC50=30 nM), upregulates 15-lipoxygenase-1, induces fetal hemoglobin, from C. carbonum.</p>

<p>H3B-8800 is an SF3B1 modulator that can be used to study transfusion-dependent anemia.</p>

<p>8-hydroxy Efavirenz, a main efavirenz metabolite by CYP2B6, causes apoptosis in rat neurons at 0.01 μM.</p>

Mepacrine (Erion) is an acridine derivative formerly widely used as an antimalarial.

<p>PAK4-IN-3 (compound 27e) is a PAK4 inhibitor exhibiting an IC50 of 10 nM and demonstrates antiproliferative effects on A549 cells with an IC50 of 0.61μM.</p>