Apoptosi

<p>Conglobatin is a natural product for research related to life sciences. The catalog number is T36494 and the CAS number is 72263-05-9.</p>

<p>WEHI-3773 is an inhibitor of the interaction between VDAC2 and either BAK or BAX. It prevents BAX-mediated apoptosis (Apoptosis) by blocking the recruitment of BAX to the mitochondria through VDAC2. Conversely, WEHI-3773 promotes BAK-mediated apoptosis (Apoptosis) by limiting VDAC2's inhibitory sequestration of BAK. This compound shows promise for research in the field of cancer therapy.</p>

<p>Peptide from c-Jun (33-57) blocks JNK binding, inhibits phosphorylation, upregulates p21, and induces HeLa cell apoptosis.</p>

<p>JNK-1-IN-3 (Compound 9e) downregulates JNK1 and phosphorylated JNK1, reduces c-Jun and c-Fos expression in tumours, and restores p53 activity.</p>

<p>Cereblon ligand for PROTAC R&amp;D; has E3 ligase, alkylC1-PEG3-alkylC3 linker, terminal amine. Part of Arvinas-licensed tool molecules.</p>

<p>Distamycin A (NSC-82150), oligopeptide antibiotic, binds A/T rich DNA, affects cleavage sites, enhances apoptosis.</p>

<p>Pralnacasan blocks IL-18, IL-1β, IFN-γ. It’s a potent oral enzyme inhibitor with use in arthritis therapy (Ki: 1.4 nM).</p>

<p>U7D-1: First-class USP7 PROTAC degrader, DC50 33 nM, anticancer, induces apoptosis in Jeko-1.</p>

<p>PLD-IN-1 (Compound 3r) is an orally effective inhibitor of phospholipase D (phospholipaseD) with an IC50 of 1.97 μM. It reduces the expression of CD24, CD47, and PD-L1 while enhancing the expression of calreticulin, thereby modulating the immune evasion mechanisms of lung cancer cells by promoting the phagocytosis of cancer cells by macrophages. PLD-IN-1 inhibits the viability of lung cancer cell lines A549, HCC44, H460, and HCC15 with IC50 values of 18.44, 22.31, 24.85, and 21.45 μM, respectively. It induces apoptosis (apoptosis) in A549 cells and inhibits cell migration. Additionally, PLD-IN-1 increases pro-inflammatory M1 macrophage levels and decreases anti-inflammatory M2 macrophage levels, exhibiting anti-tumor activity in mouse models.</p>

<p>RLX HCl is anticancer, inhibits tumour proliferation by suppressing the PI3K/Akt/FoxO3a in experimental colon cancer, antiproliferative.</p>

<p>Ledostomig is an immunoglobulin (H-γ1-scFv-L-κ) dimer monoclonal antibody that targets human neurotensin receptor type 5 (NTS5) and programmed death-1 (PD-1). It shows potential for research in various cancer types.</p>

<p>Asaretoclax is an effective inhibitor of B-cell lymphoma 2 (Bcl-2), demonstrating potential for use in cancer research.</p>

<p>EGFR-IN-131 (compound 3a) is an efficacious EGFR inhibitor capable of crossing the blood-brain barrier, with an IC50 value of 272.9 nM. This compound exhibits anti-proliferative activity, induces cellular apoptosis (apoptosis), and causes cell cycle arrest in the G0/G1 phase. Additionally, EGFR-IN-131 reduces the protein expression of p-EGFR.</p>

<p>AS-99 TFA: potent ASH1L inhibitor, IC50=0.79 μM, combats leukemia, inhibits cell growth, induces apoptosis.</p>

<p>Thalidomide-O-amido-PEG4-azide is a polyethylene glycol (PEG) derivative serving as a linker for Proteolysis Targeting Chimeras (PROTACs) synthesis [1].</p>

<p>CRA-026440 hydrochloride is a potent and broad-spectrum HDAC inhibitor.</p>

<p>3MB-PP1 is a bulky purine analog and a Polo-like kinase 1 (Plk1) inhibitor.</p>

Compound Ir5 (Antitumor agent-145) serves as a tumor inhibitor characterized by significant fluorescence and mitochondrial targeting. It promotes anti-cancer activity by inducing necroptosis and stimulating the necroptosis-related immune response [1].

<p>ICy-OH, an iodinated anticancer photosensitizer, excels in deep tissue imaging (640 nm excitation) and triggers pyroptosis in pancreatic cancer cells.</p>

<p>Cannflavin A, isolated from Cannabis sativa L., exhibits anti-cancer, neuroprotective, and anti-inflammatory activities by inhibiting Aβ1-42 aggregation and</p>

<p>SL-01, an oral gemcitabine derivative, potently induces apoptosis to hinder breast cancer more effectively than gemcitabine.</p>

<p>Hexapeptide-11 is a novel proteostasis network modulator in human diploid fibroblasts.</p>

<p>Monensin, from Streptomyces cinnamonensis, inhibits Wnt/β-catenin. Potential anticancer agent.</p>

<p>intestinal epithelium-specific growth factor</p>

<p>Indinavir is an HIV protease inhibitor,HAART. inhibits the activation of MMP-2 in endothelial cells and exhibits affinity for α7-nAchR and SARS-CoV-2 Mpro.</p>

<p>GPX4-IN-5 is a GPX4 inhibitor with antitumor activity.GPX4-IN-5 induces iron death and may be used for the treatment of triple negative breast cancer.</p>

<p>dTAG-7 selectively degrades BRD4 and FKBP12F36V by linking BET bromodomains to E3 ligase CRBN; it's a heterobifunctional degrader.</p>

<p>BT44, a potent second-gen GDNF mimetic, is a lead for treating neurodegeneration.</p>

<p>RIPK1-IN-30 (compound 24) is a potent RIPK1 inhibitor with an IC50 of 2.01 μM. It demonstrates a protective effect in the HT-29 cell model of TSZ-induced necroptosis, with an EC50 of 6.77 μM.</p>

<p>P1D-34 is a Pin1 PROTAC degrader with a DC50 value of 177 nM. It downregulates Pin1 substrate proteins, including Cyclin D1, Rb, Mcl-1, Akt, and c-Myc. Additionally, P1D-34 exhibits antiproliferative activity across various acute myeloid leukemia (AML) cell lines and induces DNA damage and apoptosis by generating reactive oxygen species (ROS).</p>

<p>MEK/PI3K-IN-2 is a potent dual inhibitor (MEK1 IC50: 352 nM, PI3Kα: 107 nM, PI3Kδ: 137 nM) that reduces pAKT, pERK1/2, and hinders tumor cell growth.</p>

<p>p53 and MDM2 proteins-interaction-inhibitor (racemic) is an inhibitor of the interaction between p53 and MDM2 proteins.</p>

<p>Cell-permeable CaM agonist; activates phosphodiesterase, binds to Ca2+ channels, inhibits cytotoxicity (IC50=52μM), protects cells, reduces inflammation.</p>

<p>PDE4B-IN-4 is an inhibitor of PDE4B (IC50: 2.82 nM) and TNF-α (IC50: 7.20 nM). It demonstrates anti-inflammatory properties by reducing neutrophilia in a mouse model of lipopolysaccharide (LPS)-induced sepsis.</p>

<p>Daporinad hydrochloride (FK 866 hydrochloride) is a NAMPT inhibitor with antitumor and antiangiogenic activity that induces apoptosis in tumor cells.</p>

<p>MDM2-IN-21 is a potent MDM2 inhibitor. MDM2-IN-21 can be used for the research of cancer.</p>

<p>TPP-1 TFA is a high-affinity PD-L1 inhibitor (KD=95nM) that boosts T-cell function to curb tumor growth.</p>

<p>JGB1741, a SIRT1 inhibitor (IC50=15µM), modulates apoptosis markers and p53 acetylation in breast cancer research.</p>

<p>PRMT5-IN-45 (compound 36) is a potent and selective inhibitor of PRMT5, exhibiting an IC50 value of 3 nM. This compound effectively reduces the levels of symmetrical dimethylarginine (sDMA) and inhibits the proliferation of the MOLM-13 cell line by inducing apoptosis and causing cell cycle arrest.</p>

<p>Zamzetoclax (compound 1) acts as a potential inhibitor of Mcl-1.</p>

<p>Arg-Gly-Asp-D-Phe-Val (TFA) has anti-tumor activity and is an inhibitor of integrin αvβ3.</p>

<p>Moflerafusp alfa is a fusion protein that targets the human signal-regulatory protein alpha (SIRPα) variant V2 D1 domain and human programmed death-ligand 1 (PD-L1). It shows potential for research in various cancer treatments.</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>A011, a potent and selective ataxia-telangiectasia mutated (ATM) inhibitor, exhibits an IC50 of 1.0 nM and triggers apoptosis as well as G2/M phase cell cycle</p>

<p>F1324: potent BCL6 inhibitor, IC50=1nM, binding t1/2=441s, strongly inhibits BCL6 PPI.</p>

<p>Thalidomide-based E3 ligase linker for PROTACs with a 3-unit PEG chain.</p>

<p>CRP protein and its fragment (174-185, RS-83277) boost human monocyte and macrophage cancer-killing effects in vitro.</p>

<p>7-epi-Isogarcinol, a PPAP, hinders STAT3 to induce apoptosis and curbs cell migration with moderate antiproliferative effects.</p>

<p>DAPK Substrate Peptide TFA is a synthetic peptide that serves as a substrate for the enzyme death-associated protein kinase (DAPK), exhibiting a Michaelis</p>

<p>PROTAC CDK4/6 degrader 1 (Compound 7f) is a dual degrader of CDK4 and CDK6, with DC50 values of 10.5 nM and 2.5 nM, respectively. This compound effectively inhibits proliferation in Jurkat cells (IC50 of 0.18 μM), induces cell cycle arrest during the G1 phase, and triggers cell apoptosis (apoptosis).</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>RPS6-IN-1 (Compound 22o) inhibits cell migration and induces apoptosis (increasing the expression of Bax, p53, cleaved-caspase 3, and cleaved-PARP). It reduces mitochondrial membrane potential and activates autophagy (Autophagy) through the PI3K-Akt-mTOR signaling pathway, damaging mitochondria and lysosomes within the cell and causing endoplasmic reticulum stress. RPS6-IN-1 also inhibits the phosphorylation of RPS6. Notably, RPS6-IN-1 is a low systemic toxicity anticancer agent.</p>

<p>Fludioxonil (CGA 173506), a phenylpyrrole fungicide, inhibits the growth of B. cinerea from strawberry and blackberry crops.</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>Nauclefine, a plant alkaloid, triggers cancer cell death through PDE3A-SLFN12, binding but not inhibiting PDE3A.</p>

<p>BRD4 Inhibitor-38 (Compound 25) is an orally active BRD4 inhibitor, exhibiting IC50 values of 3.64 μM for BRD4 BD1 and 0.12 μM for BRD4 BD2. It also demonstrates anti-inflammatory properties, with an IC50 value of 1.98 μM for nitric oxide (NO) production.</p>

<p>HDSI-18 is an orally active selective inhibitor of HDAC6 with an IC50 of 1.6 nM. It exhibits cytotoxic effects against K562, MV4-11, MOLM-13, THP-1, and Jurkat cells with IC50 values of 0.48, 0.58, 0.91, 1.79, and 4.31 μM, respectively. HDSI-18 can activate Caspase-3, induce mitochondrial depolarization, and trigger apoptosis (Apoptosis), demonstrating antitumor activity.</p>

<p>CQ-ER is a Coumarin-quinazolinone-based photosensitizer targeting the endoplasmic reticulum (ER). It induces ferroptosis, thereby enhancing photodynamic therapy (PDT).</p>

<p>MG-C-30 is an orally active CD27 agonist with an EC50 of 0.84 μM. It activates co-stimulatory signaling in NK cells and T cells, thereby enhancing the immune response. In the EG7-OVA mouse model, MG-C-30 demonstrates antitumor activity.</p>

<p>Human PD-L1 inhibitor I, a peptide, blocks PD-L1/PD-1 interaction with 3.39 μM affinity.</p>

<p>Human PD-L1 inhibitor II is a potent PD-L1 inhibitor with anti-cancer activity.</p>

<p>Xerophilusin B from Isodon xerophilus halts ESCC cell growth, causes G2/M arrest, and induces apoptosis.</p>

<p>Curzerene, a sesquiterpene compound derived from the rhizome of Curculigo orchioides Gaertn, possesses potent anti-cancer properties.</p>

<p>Oligomycin B is an antibiotic isolated from marine Streptomyces, is an eukaryotic ATP synthase inhibitor, induces apoptosis.</p>

<p>Stem bromelain: cysteine protease from pineapple stem with fibrinolytic, anti-inflammatory, antitumoral properties.</p>

<p>BMSpep-57: Macrocyclic peptide, inhibits PD-1/PD-L1, IC50=7.68 nM, binds PD-L1 (Kd=19 nM/MST, 19.88 nM/SPR), boosts T cell IL-2 in PBMCs.</p>

<p>TopoisomeraseI/II inhibitor 6 (compound 3i) acts as an effective inhibitor of topoisomerase I and II, with IC50 values of 4.77 µM and 15 µM, respectively. Additionally, it exhibits antiproliferative activity against the human melanoma cell line LOX IMVI, demonstrating IC50 values of 26.7 µM and 25.4 µM.</p>

<p>Thalidomide-5-PEG2-Cl is a cereblon ligand that recruits CRBN protein and forms PROTACs through linker conjugation.</p>

<p>PROTACNCOA4 degrader-1 (Compound V3) is a PROTAC-based degrader of NCOA4, exhibiting a DC50 of 3 nM in HeLa cells. Besides acting as a ferroptosis inhibitor, this compound effectively reduces the levels of NCOA4 and decreases intracellular ferrous (Fe2+) levels. Moreover, PROTACNCOA4 degrader-1 ameliorates liver damage in a CCl4-induced acute liver injury model.</p>

<p>Azurin p28 peptide, a tumor-penetrating antitumor agent, stabilizes p53 by reducing its proteasomal degradation via the formation of a p28:p53 complex.</p>

<p>Peptide is p53's amino acids 17-26, contacts Mdm-2 binding domain, also called p53N.</p>

<p>XIAP BIR2/BIR2-3 inhibitor-1 (compound 3) serves as a potent dual inhibitor targeting BIR2 and BIR2-3 domains, with IC50 values of 1.9 nM and 0.8 nM, respectively. This compound is utilized in cancer research studies [1].</p>

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

<p>RETligand-1 is a target protein ligand that specifically interacts with RET and can be utilized in the synthesis of the PROTAC LDD39.</p>

<p>TS-24 is a cysteine protease histone S (CTSS) inhibitor that promotes BRCA1-mediated apoptosis.</p>

<p>ATPase-IN-3 is an ATPase (ATPase) inhibitor that can be used in the study of metabolism-related diseases.</p>

<p>Claturafenib is a brain-permeable, selective, all-mutant BRAF inhibitor.PF-07799933 has shown antitumor activity, used in combination with MEK inhibitors.</p>

<p>Thalidomide-O-C8-COOH, also known as Cereblon ligand 3, is a Thalidomide-derived compound that serves as a Cereblon (CRBN) ligand for the targeted recruitment</p>

<p>AP1867-2-(carboxymethoxy), a moiety based on the synthetic FKBP12F36V-directed ligand AP1867, connects to the CRBN ligand through a linker to generate dTAG</p>

<p>Nemorosone, a PPAP from C. rosea, inhibits neuroblastoma and pancreatic cancer cell growth, induces apoptosis, and reduces mouse xenograft tumors.</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>Golimumab (CNTO-148), an anti-TNFα IgG1κ monoclonal antibody with anti-inflammatory and anti-cancer activity, can be used to prevent inflammation and cartilage.</p>

<p>PROTAC EZH2 Degrader-3 (compound ZJ-20) is a potent EZH2 degrader that exhibits strong inhibitory effects not only on EZH2 protein expression but also on the levels of other PRC2 subunits and H3k27me3 protein. Additionally, PROTAC EZH2 Degrader-3 demonstrates antiproliferative activity by blocking the cell cycle at the G0-G1 phase and inducing apoptosis (cell death). At a concentration of 5 μM and over a period of 24 hours, it effectively suppresses the expression of these critical proteins involved in cell regulation and growth.</p>

<p>Terrain (NSC 291308), a fungal metabolite, reduces age-related inflammation via Nrf2/ERK1/2/HO-1 and inhibits IL-6 in human fibroblasts.</p>

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

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

<p>DH-18 is an inhibitor of matrix metalloproteinase-2 (MMP-2), exhibiting IC50 values of 139.45 nM for MMP-2, 518.11 nM for MMP-9, and 833.34 nM for MMP-8. The compound promotes cell apoptosis and causes cell cycle arrest in the G0/G1 phase. DH-18 also inhibits cell growth, making it potential for research in chronic myeloid leukemia.</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>

<p>Antiproliferative Agent-42 (Compound 7m), a dihydrodipyrrolo compound, exhibits antiproliferative activity against the Panc-1 cell line, with an IC 50 of 12.54</p>

<p>Tubulysin B: a potent, cytotoxic microtubule-disrupting peptide from Archangium geophyra and Angiococcus disciformis.</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>CDK-TCIP1 is a bivalent molecule that links the CDK9 inhibitor SNS-032 with the BCL6 ligand BI3812. It effectively and specifically kills cells overexpressing BCL6, with an EC50 of 7.7 nM for SUDHL5 cells.</p>

<p>MG-277 is a molecular glue compound transformed from PROTAC degradation agent, MG-277 potently inhibits tumor cell growth in a p53-independent manner.</p>

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

<p>Pipermethystine is a useful organic compound for research related to life sciences and the catalog number is T124340.</p>

<p>IRF1-IN-1 (Compound I-2) is an IRF1 inhibitor , inhibiting the cleavage of Caspase 1, GSDMD, IL-1, and PARP1,protecting against skin inflammatory damage.</p>

<p>YF135 is a reversible-covalent KRAS G12C PROTAC that degrades its target via the VHL-proteasome pathway.</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>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>