Apoptosi

<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>

<p>Ub4ix, a DUB/26S proteasome inhibitor, safeguards K48-linked Ub chains against cleavage by deubiquitinating enzymes (DUBs) and inhibits the proteasomal degradation of Ub-tagged proteins. Additionally, it diminishes the viability of Hela cells and triggers apoptosis, exhibiting an IC 50 value of 1.6 μM.</p>

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

<p>Thalidomide-Piperazine-PEG2-NH2 is a synthetic E3 ligase ligand-linker for PROTAC, combining cereblon ligand with a PEG2 linker.</p>

<p>D-Trimannuronic acid from seaweed induces TNF-α in mouse macrophages; useful in pain, dementia studies.</p>

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

<p>Pamlectabart is a humanised antibody targeting TNFRSF17/BCMA, (ADC) Pamlectabart tismanitin multiple myeloma.</p>

<p>Varlilumab (CDX-1127) is a novel human IgG1 anti-CD27 monoclonal antibody. Varlilumab has antitumor activity and can be used to study advanced solid tumors.</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>Thevetiaflavone, a natural flavonoid from W. indica, blocks LDH leakage, boosting cell survival.</p>

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

<p>CRM1-IN-2 (Compound KL2) is a noncovalent inhibitor that targets CRM1, localizing it to the nuclear periphery, depleting its nuclear presence, and inhibiting</p>

<p>H-20 is a PD-1 agonist that reduces the required dosage of morphine for analgesia. It can be used in studies related to chronic pain.</p>

DB0614 degrades 26 kinases including AAK1 and CDK6, targeting aberrant activity in disease research.

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

<p>(Iso)-Z-VAD(OMe)-FMK is an isomer of Z-VAD(OMe)-FMK, which is a pan-caspase inhibitor with irreversible properties. Z-VAD(OMe)-FMK is also an inhibitor UCHL1.</p>

<p>1-(4-chloro-3-(trifluoromethyl)phenyl)-3-(7-(1-methyl-1H-pyrazol-4-yl)-2,3,4,9-tetrahydro-1H-carbazol-3-yl)urea 是一种能够激动 TNF-α的化合物，可以诱导细胞分泌 TNF-α。</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>2,2-Dimethyl-2,3-dihydrobenzofuran-7-ol inhibits the proliferation of the THP-1 cell line and anti-infective Leishmania and Toxoplasma gondii RH.</p>

<p>Platycoside G3 is a useful organic compound for research related to life sciences. The catalog number is T124100 and the CAS number is 849758-44-7.</p>

<p>MMRi62, a MDM2-MDM4 inhibitor, induces ferroptosis and autophagy in PDAC, degrades FTH1 and mutant p53, and inhibits KRAS/TP53 mutant PDAC in mice.</p>

<p>Nrf2 activator 19 is a compound capable of crossing the blood-brain barrier and acts as an NRF2/HO-1 activator, offering potent antioxidant and neuroprotective effects. It effectively reduces brain damage and minimizes the accumulation of Reactive Oxygen Species (ROS). Additionally, Nrf2 activator 19 inhibits neuronal apoptosis, aiding in the recovery of neural function and motor skills. It has demonstrated significant potential in ischemic stroke research.</p>

<p>Apoptosisinducer 26 (compound [AgCl(dap2SH)(PPh3)2]) is a mononuclear Ag(I) ligand-based autophagy inducer that exhibits antibacterial and anticancer activities against various bacterial strains and cancer cell lines. This compound facilitates the accumulation of Ag(I) ions in the periphery of bacteria, effectively inhibiting the growth of both Gram-positive (+) and Gram-negative (-) bacteria. Additionally, Apoptosisinducer 26 can intercalate between the base pairs of CT DNA, inducing apoptosis in A549 cells. It also possesses radical scavenging properties, which helps prevent oxidative stress.</p>

Human TNF alpha (46-65) peptide.

<p>p53-Mdm2 inhibitor 4 inhibits the p53-MDM2 protein-protein interaction.</p>

<p>Z-LEHD-FMK is a selective and potent caspase-9 inhibitor that protects against reperfusion injury and slows apoptosis.Z-LEHD-FMK exhibits antitumor and</p>

<p>Rasfonin, a fungal metabolite from T. terrophilus, halts mouse splenocyte growth; IC50: 0.7 μg/ml (ConA), 0.5 μg/ml (LPS).</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>

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

<p>ZX782 acts as a GPX4 protein degrader and an inducer of ferroptosis (Ferroptosis), targeting GPX4 for destruction via both the ubiquitin-proteasome system and the autophagy-lysosome pathway. Following the degradation of GPX4 induced by ZX782, there is a significant increase in the accumulation of lipid reactive oxygen species (ROS) in HT1080 cells.</p>

<p>VEGFR-2-IN-66 (Compound 6) is an orally active VEGFR-2 inhibitor with an IC50 of 0.509 µM and an IC50 value of 7.48 μM for inhibiting MCF-7 cell proliferation. Its anticancer activity is exerted through cell cycle arrest, induction of apoptosis (Apoptosis), and modulation of gene expression, making it suitable for breast cancer research.</p>

<p>SLF TFA, a synthetic FKBP ligand, binds FKBP51 (3.1 μM) and inhibits FKBP12 (IC50 2.6 μM); used in PROTAC synthesis.</p>

<p>(D)-PPA 1 TFA is a hydrolysis-resistant D-peptide antagonist and a potent PD-1/PD-L1 inhibitor, exhibiting an affinity for PD-1 of 0.51 μM and demonstrating</p>

<p>HPOB is an effective and specific HDAC6 inhibitor (IC50: 56 nM), &gt;30-fold selectivity over other HDACs.</p>

<p>PI3Kα-IN-14 (compound F8), a potent PI3Kα inhibitor, exhibits an IC50 value of 0.14 nM and markedly diminishes mitochondrial membrane potential, resulting in</p>

<p>(R)-1-(2-((2-MeO-4-(piperazin-1-yl)phenyl)amino)pyridin-4-yl)-N-(4-(CF3O)benzyl)piperidine-3-carboxamide HCl is anti-apoptotic and anti-cancer.</p>

<p>W1131 TFA is a STAT3 inhibitor and ferroptosis inducer that regulates the IL6-JAK-STAT3 and ferroptosis pathways,gastric cancer.</p>

<p>Thalidomide-O-amido-C6-NH2 is a synthetic E3 ligase used for PROTAC creation, containing cereblon ligand and linker.</p>

<p>Z-VDVA-(DL-Asp)-FMK is a derivative compound of Z-VDVAD-FMK specifically designed as an inhibitor targeting caspase-2.</p>

GPI-1485 (GM1485) (GM1485) is a nonimmunosuppressive immunophilin ligand, promoting neurofunctional improvement and neural regeneration following stroke.

<p>Apoptolidin, from Nocardiopsis, induces apoptosis, targets mitochondrial ATPase (Ki 4-5 μM), kills glial cells, and has antibiotic and antifungal properties.</p>

<p>Carbonic anhydrase inhibitor33 (11D) is a dual inhibitor that targets both CA (carbonic anhydrase) IX/XII and CDK6. It exhibits Ki values of 19.7 nM for hCA IX and 26.1 nM for hCA XII. Additionally, Carbonic anhydrase inhibitor33 (11D) can induce G1 phase cell cycle arrest and apoptosis, making it relevant for research in non-small cell lung cancer (NSCLC).</p>

<p>HDAC3-IN-6 (Compound SC26) is a selective HDAC3 inhibitor with an IC50 of 53 nM. It induces PD-L1 expression in a dose-dependent manner and leads to significant apoptosis and reactive oxygen species (ROS) production. HDAC3-IN-6 exhibits strong antitumor efficacy against colorectal cancer.</p>

<p>PD-L1/LpxC-IN-1 (Compound 12b) is an inhibitor of PD-L1 and LpxC, with IC50 values of 5.2 μM and 0.081 μM, respectively. This compound disrupts bacterial lipopolysaccharide biosynthesis, leading to bacterial cell lysis and death. It effectively inhibits Gram-negative bacteria, exhibiting a minimum inhibitory concentration (MIC) of 0.25-0.5 μg/mL against K. pneumoniae ATCC 13883, E. coli ATCC 8739, S. typhimurium ATCC 14028, and P. aeruginosa ATCC 9027. Additionally, PD-L1/LpxC-IN-1 modulates the immune response by downregulating the expression of inflammatory cytokines IL-2 and IFN-γ, and upregulating CD4+ and CD8+ cells, thus activating the immune system and mitigating excessive inflammatory responses. In a mouse model of K. pneumoniae ATCC 13883 infection, PD-L1/LpxC-IN-1 demonstrated antibacterial activity.</p>

<p>Caspase-3 inhibitor. Inhibits MG 132-induced small cell lung cancer cell death in vitro.</p>

<p>Dc-y13-27, a derivative of DC-Y13, is a potent YTHDF2 inhibitor (KD: 37.9 μM).</p>

<p>Epoprostenol sodium (Prostaglandin I2 sodium salt) is a vasodilator and a synthetic prostacyclin that can be used to study pulmonary hypertension.</p>

<p>Tyroserleutide HCl, a tripeptide from pig spleen, inhibits tumor growth in vivo/vitro.</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>RBN013209 is a potent CD38 inhibitor. RBN013209 is useful in the treatment of cancer.</p>

<p>DTUN: lipophilic radical initiator, starts STY-BODIPY liposome co-autoxidization at 0.2 mM, useful in FENIX assays.</p>

GPLGIAGQ, a MMP2-cleavable polypeptide, is used as a stimulus-sensitive linker in both liposomal and micellar nanocarriers for MMP2-triggered tumor targeting.

<p>Tralokinumab: human IgG4 monoclonal antibody, blocks IL-13, may treat atopic dermatitis.</p>

<p>EAD1 is a useful organic compound for research related to life sciences. The catalog number is T35329 and the CAS number is 1644388-26-0.</p>

<p>5α-dihydro Levonorgestrel is a metabolite of the synthetic progestin levonorgestrel .</p>

<p>Vorsetuzumab (Anti-Human CD70 Recombinant Antibody) is a monoclonal antibody targeting the CD70 antibody.</p>

<p>Peginterferon beta-1a: first pegylated interferon for cancer, RMS research; induces tumor cell apoptosis.</p>

<p>2-Acetamidophenol (Orthocetamol) has analgesic and antipyretic effects. 2-Acetamidophenol is an isomer of Paracetamol (4-acetamidophenol).</p>

<p>Oxatomide: Dual H1/P2X7 antagonist, antihistamine, anti-allergic, treats immune diseases, IC50: 0.95 μM (P2X7), 0.43 μM (5-HT).</p>

<p>WKYMVM is a N-formyl peptide receptor (FPR1) agonist.</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>eIF4A3-IN-5 potently inhibits eIF4AI/II, promising for cancer research.</p>

<p>KC01 selectively inhibits ABHD16A (IC50: 0.2-0.5 μM), much more potent than KC02 (&gt;10 μM); human ABHD16A IC50: 90±20 nM.</p>

<p>Mcl-1 Inhibitor 16 (Compound 9), a platinum-based mitochondrial-targeting agent, inhibits Mcl-1 and induces Bax/Bak-dependent apoptosis in cancer cells.</p>

<p>Ono 3403, a synthetic serine protease inhibitor, blocks TNF-alpha, NO production, and has antitumor properties.</p>

<p>Verdinexor (KPT-335) (KPT-335), a specific XPO1/CRM1 inhibitor, are orally bioavailable.</p>

<p>Raptinal activates caspase-3 directly and initiates intrinsic caspase-dependent apoptosis pathway in multiple cell lines.</p>

<p>F1324 TFA is a potent, high affinity peptidic inhibitor of B cell lymphoma 6 (BCL6), with an IC50 of 1 nM.</p>

<p>Rozanolixizumab (RYSTIGGO) is a humanized IgG4 monoclonal antibody that targets FcRn in newborns for autoimmune research.</p>

<p>KB03-SLF is a protease with the capability to target specific proteins and regulate intracellular protein levels by inducing protein degradation. This mechanism renders KB03-SLF potentially valuable in the suppression of related diseases.</p>

<p>EPZ020411 hydrochloride is a selective and potent small molecule PRMT6 inhibitor with an IC50 value of 10 nM.</p>

<p>Mofarotene (Ro-40-8757) is a small molecule compound that shows considerable antitumor activity in many cancer cell lines and can be used for the treatment of</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>Azadirone, a limonoid, sensitizes cancer cells to TRAIL by modulating DR4/DR5, survival, and apoptotic proteins.</p>

RET-IN-28 (Compound 16) is an inhibitor of RET (a transmembrane receptor tyrosine kinase). It specifically inhibits the activity of a mutant RET enzyme (RET-V804M) and is utilized in cancer research.

NQO2-IN-1, a resveratrol analog, is a potent NQO2 inhibito,antitumor,generation of ROS and up-regulation of DR5 (death receptor 5) to promote apoptosis.

<p>Sotigalimab (APX 005) is a monoclonal antibody targeting CD40 with anticancer activity for the study of metastatic pancreatic cancer.</p>

<p>NC-R17, an RSL3-based noncovalent GPX4 degrader implicated in ferroptosis, demonstrates anti-tumor activity and is utilized in the design of noncovalent GPX4-</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>Delmitide, a TNF-alpha production inhibitor, is used potentially for the treatment of Crohn's disease and ulcerative colitis.</p>

<p>RvD2 n-3 DPA is an SPM made from docosapentaenoic acid in human leukocytes, inhibiting neutrophil chemotaxis and adhesion.</p>

Bcl-2-IN-5: BCL-2 inhibitor, IC50: 0.12 nM (wt), 0.14 nM (D103Y), 0.22 nM (G101V); Cell growth IC50: 0.2 nM, 0.44 nM (RS4;11).

<p>TD52 dihydrochloride, an Erlotinib derivative, inhibits protein phosphatase 2A and induces apoptosis in TNBC by disrupting CIP2A/PP2A/p-Akt signaling.</p>

<p>Amino-PEG6-Thalidomide is a PEG-based linker for PROTACs which joins two essential ligands, crucial for forming PROTAC molecules.</p>

<p>HTR2A antagonist 1 (Compound 15f) is an HTR2A antagonist with an IC50 of 42.79 nM. It induces sub-G1 cell cycle arrest and apoptosis in colorectal cancer cells by activating the p53/p21/caspase 3 signaling pathway. HTR2A antagonist 1 exhibits good liver microsomal stability and is useful for colorectal cancer research.</p>

<p>TD1092, a pan-IAP degrader, activates caspase 3/7, induces apoptosis in cancer cells, inhibits NF-κB, and is used in cancer research.</p>

<p>2,4,6-trichloroanisole inhibits the cell viability of CHO and C32 cell lines and apoptosis, antibacterial activity against Plasmodium falciparum.</p>

<p>SC-2001 inhibits MCL-1 and STAT3, enhances SHP-1, induces apoptosis in breast cancer, and counters STAT3-driven sorafenib resistance in liver cancer.</p>

<p>HEMTAC CDK4/6 degrader 1, a PROTAC targeting HSP90/CDK4/6, Kd of 35.7 μM, disrupts B16F10 melanoma cell cycle, and induces apoptosis.</p>

<p>Bcl-B inhibitor 1 is a Bcl-B inhibitor with antitumor activity that binds to and inactivates pro-apoptotic proteins in the BH3 structural domain.</p>

YJ1206 is a highly potent and selective CDK12/13 PROTAC degrader oral, DNA damage and cell-cycle arrest,and inhibits the proliferation of prostate cancer cells.

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

<p>1-Methyl-1H-pyrrolo[2,3-b]pyridine exhibits cytotoxicity against MCF-7 cells and can be used in related research in the field of life sciences.</p>

<p>PPIA-IN-1 (Compound 20b) is an inhibitor of peptidyl-prolyl isomerase A (PPIA) with a KD of 0.52 μM. It demonstrates antiproliferative activity across various cancer cell lines, including an IC50 of 0.69 μM in HCT116 cells, induces cell cycle arrest at the G0/G1 phase, and exhibits antimetastatic effects in HCT116 cells. PPIA-IN-1 elevates ROS levels, causing DNA damage, ER stress, and mitochondrial dysfunction, and induces apoptosis in HCT116 cells via the MAPK pathway. Additionally, PPIA-IN-1 shows antitumor activity in a CT26 xenograft mouse model.</p>

<p>Compound 6b is a synthetic Thalidomide-VHL E3 ligase-linker for PROTACs.</p>

<p>Fludioxonil (CGA 173506), a phenylpyrrole fungicide, inhibits the growth of B. cinerea from strawberry and blackberry crops.</p>

<p>Aspochalasin D, isolated from A. microcysticus, shows antibacterial properties and cytotoxicity affecting Ba/F3-V12 cells, with IC50s of 0.49 and 1.9 μg/ml.</p>

<p>The compound is a negative control peptide for the Bax inhibitor peptides V5 and P5.</p>

<p>EGFR-IN-153 (Compound 5l) is an EGFR inhibitor that suppresses the proliferation of MDA-MB-231 cells with an IC50 of 0.73 μM and induces apoptosis. It is applicable for research in breast cancer.</p>

<p>BU 224 hydrochloride is a selective imidazoline I(2) binding site ligand and has antinociceptive and antidepressant-like activities.</p>

<p>Desmethyl-WEHI-345 analog, a protein kinase inhibitor, holds potential for colon cancer research.</p>

<p>AKT-IN-18, an Akt inhibitor, demonstrates an IC50 value of 69.45 μM in A549 cells, effectively impeding Akt activity.</p>

<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>