Apoptosis

<p>PROTAC RIPK degrader-2 is a nonpeptidic PROTAC ,and potently targets serine-threonine kinase RIPK2 and has highly selective for RIPK2 degradation.</p>

<p>(R)-MIK665 is the less active enantiomer of MIK665. MIK665 is a special inhibitor of Mcl-1(IC50 of 1.81 nM).</p>

<p>Flu-BakBH3 peptide, derived from Bak's BH3 domain, binds tightly to a crucial pocket of Bcl-XL, essential for its anti-death role.</p>

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

<p>Ascochlorin, an isoprenoid antibiotic, inhibits STAT3 to combat tumors, induces apoptosis, and reduces inflammation.</p>

<p>Psalmotoxin 1 is a potent and selective acid-sensing ion channel 1a (ASIC1a) blocker.</p>

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

<p>Compound 29c, a Thalidomide-linker conjugate for potent PROTAC BRD2/BRD4 degrader-1, targets BET proteins.</p>

<p>Opamtistomig is a humanized monoclonal antibody immunoglobulin (H-γ1-scFv-L-κ) dimer targeting human programmed death-ligand 1 (PD-L1), CD274, and tumor necrosis factor receptor superfamily member 9 (TNFRSF9). It is anticipated for use in research on various solid tumors and hematologic malignancies.</p>

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

<p>YF135 is a reversible-covalent KRAS G12C PROTAC that degrades its target via the VHL-proteasome pathway.</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>INF200 (compound 5), a sulfonylurea-based inhibitor of NLRP3 and associated pyroptosis, exhibits cardiometabolic benefits in a rat model of high-fat diet (HFD)-</p>

<p>Boc-AEVD-CHO, a selective Caspase 8 inhibitor, facilitates apoptosis research and the investigation of immune and inflammatory diseases [1] [2].</p>

<p>PROTACGPX4 degrader-4 is a GPX4 PROTAC degrader with a DC50 of 5.32 nM. It inhibits the activity of cancer cell lines RT4, T24, and J82 with IC50 values of 0.09, 2.97, and 7.58 μM, respectively. This compound elevates lipid ROS levels and induces ferroptosis in T24 and RT4 cells. In T24 tumor-bearing BALB/c nude mouse models, PROTACGPX4 degrader-4 demonstrates antitumor activity. It is applicable to bladder cancer research.</p>

<p>UBX1325, a potent Bcl-xL inhibitor, induces cell death in aging cells, useful for age-related eye disease research.</p>

<p>FKBP12 Ligand-Linker Conjugate 1 is a complex comprising a target protein ligand for FKBP12 and a linker, which is utilized in the synthesis of the PROTAC degrader MC-25B.</p>

<p>LY3415244 is a human bispecific antibody (bsAb) that targets B7-H1/PD-L1/CD274 and TIM-3/HAVCR2/CD366. This compound is applicable in the study of advanced solid tumors.</p>

<p>SP3N hydrochloride is a specific degrader of the prolyl isomerase (FKBP12). Its alkylamine moiety is metabolized into an active aldehyde (SP3CHO), which recruits the SCFFBXO22 ligase for the degradation of FKBP12. SP3N hydrochloride is applicable in cancer research.</p>

<p>dTAG-47 targets FKBP12 F36V for protein degradation, useful in basal-like breast cancer research.</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>Lincydomine relaxes smooth muscles, treats unstable angina, and opens human and guinea pig respiratory tracts.</p>

<p>Diazepinomicin, from Micromonospora, blocks EGF-Ras-ERK pathway and induces apoptosis; an anti-tumor agent for K-Ras mutants.</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>LH1307 blocks PD-1/PD-L1 interaction, IC50 = 3 nM (HTRF assay), activates Jurkat cells, EC50s: 79 nM (U2OS), 763 nM (CHO).</p>

<p>Thalidomide-NH-C8-NH2 is a synthetic E3 ligase ligand-linker for PROTAC, combining cereblon ligand and a specific linker.</p>

<p>Anti-inflammatory agent 42 has anti-inflammatory activity and inhibits the expression of TNF-α and IL-6 in LPS-stimulated macrophages.</p>

<p>HDAC-IN-88 (Compound HJ-9) is a potent inhibitor of HDAC, effectively targeting HDAC6, HDAC1, HDAC2, HDAC8, and HDAC3 with IC50 values of 0.226, 1.103, 2.308, 3.255, and 3.864 μM, respectively. This compound suppresses the proliferation of cancer cells HepG2, HCT116, and MV4-11 with IC50 values of 5.47, 9.78, and 0.38 μM, respectively. Additionally, it inhibits the migration of HCT116 cells, causes cell cycle arrest at the G0/G1 phase, and induces apoptosis and autophagy in MV4-11 cells. HDAC-IN-88 reduces ROS levels and mitochondrial membrane potential and demonstrates antimalarial activity by inhibiting Plasmodium falciparum 3D7 with an EC50 of 165 nM. Furthermore, HDAC-IN-88 exhibits anti-angiogenic properties.</p>

<p>AlbA-DCA, a compound of Albiziabioside A and dichloroacetate, boosts ROS and reduces lactic acid in tumors, killing cancer cells and triggering apoptosis.</p>

<p>Oxybenzone-d3 (Benzophenone 3-d3) is a deuterium-labeled form of Oxybenzone. Commonly used as a UV filter in tanning and skin protection products, Oxybenzone (Benzophenone 3) acts as an endocrine-disrupting chemical (EDC) that can cross both the placental and blood-brain barriers. It impairs autophagy, alters epigenetic states, and disrupts retinoid X receptor signaling in apoptotic neuronal cells.</p>

<p>Targaprimir-96 TFA is a selective inhibitor of miR-96 in cancer, inducing apoptosis with high affinity for pri-miR-96 but not affecting healthy cells.</p>

<p>Deoxynyboquinone is a potent inducer of cancer cell death with IC(50) values between 16 and 210 nM.</p>

<p>Bleomycin A5, or Pingyangmycin, is an oral glycopeptide antibiotic and acts as an antineoplastic and apoptosis inducer.</p>

<p>Tubulin polymerization-IN-45, a tubulin-targeting agent, acts as a tubulin polymerization inhibitor by binding to the tubulin's colchicine site.</p>

<p>Anti-TNBC agent-9 (Compound 3as) is an anticancer agent used for treating triple-negative breast cancer (TNBC). It exhibits significant inhibitory activity against MDA-MB-453 cells, with an IC50 value of 8.5 μM. Anti-TNBC agent-9 impedes tumor cell migration by upregulating E-cadherin and downregulating N-cadherin, matrix metalloproteinase 2 (MMP2), and MMP9. Additionally, it inhibits tumor cell proliferation by inducing apoptosis, achieved through the increased expression of pro-apoptotic protein BAX and decreased expression of anti-apoptotic protein BCL-2.</p>

<p>Anti-inflammatory agent 95 (Compound 2e) is a compound with potent anti-inflammatory properties, showing significant inhibition of NO production in LPS-induced RAW 264.7 mouse macrophages, with an IC50 of 8.8 μM. It also effectively suppresses the secretion of TNF-α and IL-1β, achieving inhibition rates of 60% and greater than 90% at 100 μM, respectively. Anti-inflammatory agent 95 holds promise for research into inflammatory diseases.</p>

<p>BRD-810 is a highly selective MCL1 inhibitor (Kd=0.3 nM) capable of inducing tumour cell apoptosis, for haematological malignancies and solid tumours.</p>

<p>Tubulysin B: a potent, cytotoxic microtubule-disrupting peptide from Archangium geophyra and Angiococcus disciformis.</p>

<p>MS105 is an orally active, selective protein tyrosine kinase 6 (PTK6) PROTAC degrader. It recruits the VHL E3 ligase through a VHL ligand fragment, facilitating ubiquitination and proteasomal degradation of PTK6, thereby inhibiting the proliferation and migration of breast cancer cells and inducing apoptosis (apoptosis). MS105 is a promising compound for breast cancer research.</p>

<p>FR900359 is a macrocyclic Gq protein inhibitor that inhibits melanoma cell proliferation and can be used to study asthma, inflammation and cancer.</p>

<p>CUR5-8: potent, oral CUR analog, reduces lipid droplets, boosts autophagy, hinders apoptosis, enhances insulin sensitivity.</p>

<p>PARP1-IN-17 is an inhibitor that targets PARP-1 (IC50=19.24 nM ) with a slightly reduced affinity for PARP-2 (IC50=32.58 nM ) and induces apoptosis.</p>

<p>KRAS inhibitor-40 (Compound 41) is an inhibitor of KRAS, disrupting the KRAS G12C-BRAF complex and suppressing the phosphorylation of the downstream ERK signaling pathway. This compound also inhibits the proliferation of tumor cells with various KRAS mutations, exhibiting antitumor activity.</p>

<p>YX-02-030M is a PROTACMDM2 degrader. It inhibits the binding of MDM2 to p53 and VHL to HIF1α, with IC50 values of 63 nM and 1.35 μM, respectively. YX-02-030M binds to MDM2 and recruits the VHL E3 ubiquitin ligase to initiate MDM2 degradation, effectively killing p53 mutant or deficient triple-negative breast cancer (TNBC) cells.</p>

<p>Anticancer Agent 157 (compound 15) is a nitric oxide (NO) inhibitor with IC50 values of 0.62 μg/mL, exhibiting both anti-inflammatory and anticancer effects.</p>

<p>Thalidomide-5-propoxyethanamine acts as a cereblon (CRBN) ligand derived from Thalidomide, and it serves the purpose of recruiting the CRBN protein.</p>

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

<p>dFKBP-1 is a potent and PROTAC-based FKBP12 degrader. dFKBP-1 incorporates the ligand SLF of FKBP12, the Thalidomide based cereblon ligand and a linker[1].</p>

<p>pdTp is a highly selective, small-molecule miRNA regulatory complex RISC subunit SND1 inhibitor.</p>

<p>Enniatin A1, a cyclic hexadepsipeptide from Fusarium, induces apoptosis and disrupts ERK, inhibiting ACAT (IC50: 49 μM).</p>

<p>Episilvestrol is a derivative of silvestrol with eIF4A-targeted antitumor properties, found in Aglaia silvestris fruits and twigs.</p>

<p>Reveromycin A from Streptomyces sp. inhibits epidermal growth, tumors, and C. albicans; affects osteoclasts. IC50: 0.7-1.9 μg/ml; MIC: 2 μg/ml.</p>

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

<p>BM-1244 is a potent Bcl-xL/Bcl-2 inhibitor with Kis of 134 and 450 nM for Bcl- xL and Bcl-2, respectively.</p>

<p>Destruxin B: cyclic peptide from Metarhizium fungus, induces apoptosis in lung cancer via mitochondrial pathway.</p>

<p>Hematein blocks Akt/PKB, Wnt signaling, promotes apoptosis in lung cancer, is a dye from hematoxylin, and inhibits casein kinase II (IC50: 0.74 μM).</p>

<p>PAA5, a polynuclear Au(I) cluster, triggers ferroptosis and has anticancer effects by increasing pH2AX over time.</p>

<p>AXL/Angiokinase-IN-1 (compound 11b) is an inhibitor of AXL/triple angiokinase, with an IC50 of 3.75 nM for AXL expression. This compound suppresses epithelial-mesenchymal transition (EMT) in Bxpc-3 cells and prevents metastasis in lung cancer cells. Additionally, AXL/Angiokinase-IN-1 impairs the functions of vascular and fibroblast cells and induces apoptosis in both cancer and fibroblast cells. It is characterized by low toxicity and favorable metabolic stability.</p>

<p>mTORinhibitor-27 (Compound 7e) is an inhibitor of mammalian target of rapamycin (mTOR) with an IC50 value of 5.47 μM. It can induce apoptosis in tumor cells and arrest the cell cycle in the S phase, thereby inhibiting cancer cell growth. mTORinhibitor-27 presents potential for research in cancer, including skin cancer.</p>

<p>RETligand-3 is the ligand for PROTAC QZ2135, which targets RET.</p>

<p>Suramin is an RdRp and PTPase inhibitor with anti-parasitic, anti-tumor, and anti-angiogenic activities, inhibiting sirtuins and DNA topoisomerase II.</p>

<p>C-Peptide 1 (rat) is a polypeptide isolated from proinsulin. C-Peptide acts as a β-catenin/GSK-3β activator, influences Na/K-ATPase, regulates apoptosis.</p>

<p>d-(KLAKLAK)2 is an antimicrobial and antitumor peptide, notable within the group of antimicrobial peptides, and exhibits strong anticancer properties. It kills bacteria by disrupting their cell membranes, causing leakage of cell contents. Additionally, d-(KLAKLAK)2 inhibits tumor cell proliferation by inducing apoptosis through mitochondrial swelling and membrane damage.</p>

<p>Anticancer agent 154 (Compound 8h) enhances reactive oxygen species production, causing mitochondrial damage, and promotes cell apoptosis and DNA damage.</p>

<p>SRE-II, an amide derivative, serves as an activatable photosensitizer tailored for photodynamic cancer research, exhibiting diminished fluorescence and</p>

<p>Tubulin/HDAC-IN-2 (Compound II-19k) is a dual inhibitor targeting Tubulin and HDAC, exhibiting IC50 values of 0.403 μM for HDAC1, 0.591 μM for HDAC2, 3.552 μM</p>

<p>Sterigmatocystine, a G1 phase and DNA synthesis inhibitor, curbs p21 and is a mycotoxin precursor from Aspergillus versicolor.</p>

<p>Os30 is a potent fourth-generation EGFR inhibitor, specifically targeting the EGFRC797S-TK mutation with IC50 values of 18 nM for EGFRDel19/T790M/C797S TK and</p>

<p>Thalidomide-NH-PEG7, a chemical for creating PROTAC iRucaparib-AP6, selectively degrades PARP1 and is used in ADCs.</p>

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

<p>PD-L1 inhibitor IV, a polypeptide, competitively blocks hPD-1 with a Kd of 1.38 μM, preventing hPD-1/hPD-L1 interaction.</p>

<p>Ankaflavin, from red rice fermentation, is a PPARγ agonist with anti-inflammatory properties and selectively kills cancer cells.</p>

<p>ChoKα Inhibitor-3, a sulfur-containing choline kinase inhibitor, effectively inhibits HChoK α1 with an IC50 value of 0.66 μM and possesses the capability to</p>

<p>Antitumor agent-201 (Compound 10) is a Golgi apparatus-targeting chloride ion transport activator with an EC50 for promoting transmembrane chloride ion transport of 1.53 mol% and an IC50 against HepG2 cells of 7.13 μM. By selectively acting on the Golgi apparatus, Antitumor agent-201 disrupts chloride ion homeostasis, decreases the expression of key proteins such as GM130 and GRASP55, and alters Golgi structure and function. This process induces Golgi apparatus autophagy, triggers apoptosis in cancer cells, and causes cell cycle arrest at the G2/M phase, thereby exhibiting anticancer activity. Antitumor agent-201 is applicable for research in the field of cancer-related diseases.</p>

<p>Vinepidine (LY-119863) sulfate, a derivative of vincristine, exhibits antitumor activity .</p>

<p>Rosamultic acid is a useful organic compound for research related to life sciences and the catalog number is T125342.</p>

<p>Mumefural, from Prunus mume fruit, hinders platelets, has anti-thrombotic properties, and boosts cognition.</p>

<p>Methyl-4-oxoretinoate is a synthetic retinoid with anticancer properties, used for skin conditions and potential ocular treatments.</p>

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

<p>USP1-IN-11 (compound 38-P2) is a selective, reversible, and non-competitive inhibitor of USP1 (Ubiquitin-specific protease 1). It activates the DDR (DNA damage repair) pathway, leading to cell cycle arrest and apoptosis, thereby inhibiting cell survival. USP1-IN-11 increases sensitivity to Olaparib in drug-resistant cells and works synergistically with Andrographolide in cancer cells with functional BRCA. In the MDA-MB-436 xenograft model, USP1-IN-11 demonstrates significant dose-dependent antitumor activity.</p>

<p>PROTAC RIPK degrader-6 (example 1) is a PROTAC designed for the targeted degradation of RIP Kinase, featuring a RIP2 kinase inhibitor connected through a linker</p>

<p>PROTACSMARCA2/4 degrader-38 is a SMARCA2/4 PROTAC degrader with DC50 values of 3.0 nM and 4.0 nM, respectively. It facilitates the ubiquitination and degradation of SMARCA2/4 and can block the G0/G1 phase of the cell cycle, leading to the induction of apoptosis. PROTACSMARCA2/4 degrader-38 is applicable in acute myeloid leukemia (AML) research.</p>

<p>Tubulin polymerization-IN-43 disrupts microtubules, arrests cell cycle, and induces apoptosis in leukemia by targeting colchicine sites.</p>

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

<p>IC 86621: DNA-PK ATP-competitive inhibitor, IC50 120 nM, enhances DSB antitumor effects, EC50 68 µM for repair.</p>

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

<p>3-methoxy-9H-carbazole: photosensitizer, anti-breast cancer, from Klauseneria spp., induces apoptosis.</p>

<p>PKM2 modulator 1 (compound C998) is an effective PKM2 inhibitor with antiproliferative activity. It induces apoptosis and holds potential for research in glioblastoma studies.</p>

<p>Eldecalcitol, orally active vitamin D analog, boosts bone density and treats osteoporosis.</p>

<p>4-N-Nonyloxyphenol, kaolinite nanotube photosensitizer, degrades phenolic pesticides, and disrupts endocrine.</p>

<p>LIB3S0280 is a potent inhibitor of TBK1, with an IC50 of 493.9 nM. It suppresses TBK1 downstream signaling by reducing the phosphorylation of IκBα and AKT. LIB3S0280 causes G2/M phase arrest and induces apoptosis in pancreatic cancer cells. Notably, it exhibits significant inhibitory effects on pancreatic cancer cell lines with high TBK1 expression, with a 96-hour IC50 value ranging from 6.64-10.98 μM. LIB3S0280 shows potential for research in pancreatic ductal adenocarcinoma (PDAC).</p>

<p>PD-166285 is an effective and broadly active inhibitor of protein tyrosine kinase.</p>

<p>Hydrocinchonine is an Alkaloid from Olea europaea and is found in fruits.</p>

<p>PEAQX tetrasodium hydrate: potent/selective oral NMDA antagonist, IC50 270 nM (1A/2A), 29600 nM (1A/2B).</p>

<p>Mechercharmycin A, a cytotoxic compound, was isolated from Thermoactinomyces sp. YM3-251, a marine source. It demonstrates potent antitumor activity.</p>

<p>Garivulimab (BGB-A333), a humanized IgG1 monoclonal antibody, binds to PD-L1, blocking PD-1 interaction and exhibiting antitumor activity.</p>

<p>DAPK-IN-2: DAPK inhibitor with anticancer potential. Used in cerebral infarction and ischemia research.</p>

<p>MKC-1 (Ro-31-7453) is an oral bisindolylmaleimide inhibitor that disrupts tubulin polymerization, potentially halting cancer cell division.</p>