Apoptosis

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

<p>Oligomycin B is an antibiotic isolated from marine Streptomyces, is an eukaryotic ATP synthase inhibitor, induces apoptosis.</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>DL-Sulforaphane N-acetyl-L-cysteine (SFN-NAC), induces apoptosis through α-microtubulin and phosphorylation of ERK1/2-mediated Stathmin-1, and Hsp70 (NSCLC).</p>

<p>RD-23 is an orally active and selective RET PROTAC degrader. It facilitates the ubiquitination and degradation of the RETG810C mutant with a DC50 value of 11.7 nM. Additionally, RD-23 inhibits the activation of downstream Shc signaling and induces apoptosis (Apoptosis). It is useful for studying RET-related cancers.</p>

<p>D-Trimannuronic acid from seaweed induces TNF-α in mouse macrophages; useful in pain, dementia studies.</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>DB2313 is a potent PU.1 inhibitor (IC50=14 nM) that disrupts gene binding, induces AML cell apoptosis, and has anticancer properties.</p>

<p>Nauclefine, a plant alkaloid, triggers cancer cell death through PDE3A-SLFN12, binding but not inhibiting PDE3A.</p>

<p>CSF1R-IN-26 (Compound III-1) is an inhibitor of CSF-1R with an IC50 of 20.07 nM. It promotes the polarization of M2 macrophages to M1 macrophages, inducing apoptosis in MC-38 cancer cells. CSF1R-IN-26 inhibits the activation of the AKT/ERK/STAT3 signaling pathways, remodels the tumor immune microenvironment, and exhibits antitumor activity in mouse models. In SD rats, CSF1R-IN-26 demonstrates favorable pharmacokinetic properties, with a half-life of 1.86 hours and an oral bioavailability of 79.22%.</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>Furazolidone (Furoxone), a nitrofuran derivative, inhibits AML1-ETO transformed cells with IC50 value of 12.7 μM.</p>

<p>Thalidomide-O-amido-C8-NH2 is a thalidomide-based ligand-linker for PROTAC synthesis.</p>

<p>Poly(I:C):Kanamycin (1:1) sodium is a complex.Poly(I:C) is a TLR3 and RIG-I/MDA5 agonist.Kanamycin is an antimicrobial,Gram-negative and positive bacteria.</p>

<p>BcI-2/BcI-xI ligand 1, functioning as a BcI-2/BcI-xI ligand, is utilized in the synthesis of PROTAC BcI-2/BcI-xI Degrader-1 .</p>

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

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

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

<p>RMC-7977 is a inhibitor of the active (GTP-bound) forms of KRAS, HRAS, and NRAS with anticancer activity for the study of solid tumors with KRAS G12C mutations.</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>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>PD-1/PD-L1-IN-48 (compound HD10) is an effective inhibitor of the PD-1/PD-L1 interaction, exhibiting an IC50 of 3.1 nM. It plays a vital role in cancer research.</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>Necroptosis-IN-4 is an effective inhibitor of necroptosis, specifically targeting RIP kinase 1 (RIPK1) without inhibitory activity against RIPK3. It exhibits weak inhibitory effects on VEGFR1/2 and PDGFR-α.</p>

<p>VTP50469 fumarate is a highly selective and orally active inhibitor of Menin-MLL interaction (Ki: 104 pM), and has potently anti-leukemia activity.</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>Thalidomide-O-amido-PEG4-propargyl is a polyethylene glycol (PEG)-based linker employed for the synthesis of proteolysis targeting chimeras (PROTACs)[1].</p>

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

<p>Antitumor agent-100 hydrochloride (compound A6), serving as both an apoptosis inducer and molecular glue, exhibits superior anti-tumor activity [1].</p>

<p>PI3K/HDAC-IN-4 (Compound 31f) is a dual inhibitor targeting PI3K and HDAC, with an IC50 of 0.2μM. It demonstrates high selectivity for HDAC1-3, with IC50 values of 75.5 nM, 70.9 nM, and 1.9 nM, respectively. As a potent pan-PI3K inhibitor, PI3K/HDAC-IN-4 has IC50 values of 2.5 nM, 80.5 nM, 10.0 nM, and 57.2 nM for PI3Kα, β, δ, and γ, respectively. This compound effectively induces apoptosis in tumor cells by concurrently inhibiting the PI3K/AKT/mTOR signaling pathway and HDAC1-3. It shows significant antiproliferative activity across various tumor cell lines, such as MV4-11, Jeko-1, HL60, and MCF-7, with IC50 values of 0.2, 0.9, 0.8, and 1.5 μM, respectively. PI3K/HDAC-IN-4 is applicable in the study of lymphoma and leukemia.</p>

<p>PARP1-IN-16 (compound 12a) serves as a potent PARP1 inhibitor, exhibiting an IC50 value of 1.89 nM.</p>

<p>Galloflavin Potassium is an inhibitor of lactate dehydrogenase.</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>MDM2-IN-21 is a potent MDM2 inhibitor. MDM2-IN-21 can be used for the research of cancer.</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>Etoposide phosphate disodium, a prodrug of etoposide, is a powerful anticancer drug inhibiting DNA topoisomerase II.</p>

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

<p>ElteN378: potently inhibits FKBP12 (Ki=0.5 nM), low weight, similar affinity to Rapamycin.</p>

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

<p>(R)-Q-VD-OPh is the less active enantiomer of Q-VD-OPha. Q-VD-OPha is an irreversible inhibitor of pan-caspase, with potent antiapoptotic properties.</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>CYP51/PD-L1-IN-3 (compound L21), a quinazoline with antifungal properties, serves as a dual inhibitor targeting CYP51 (IC50: 0.205 μM) and PD-L1 (IC50: 0.039 μM</p>

<p>XM-U-14 is a selective PROTAC USP7 degrader that induces the degradation of USP7 in the RS4;11 cell line with a DC50 of 0.74 nM. This compound elevates the levels of p53 and p21, and significantly inhibits the growth of acute lymphoblastic leukemia (ALL) cells, with IC50 values of 0.5 nM in RS4;11 cells and 8.3 nM in Reh cells. Moreover, XM-U-14 induces apoptosis and cell cycle arrest, and effectively inhibits tumor growth.</p>

<p>CUR5-8: potent, oral CUR analog, reduces lipid droplets, boosts autophagy, hinders apoptosis, enhances insulin sensitivity.</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>PARP1-IN-15 (Compound 6) is a PARP1 inhibitor that also inhibits tankyrase (TNKS) and promotes DNA double-strand breaks, leading to tumor cell apoptosis.</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>EGFR/COX-2-IN-1 is an EGFR/COX-2 inhibitor that effectively targets EGFRWT, EGFRT790M, COX-1, and COX-2 with IC50 values of 0.12, 0.076, 20.1, and 1.52 μM, respectively. It inhibits MCF-7, HT-29, and A-549 cells with IC50 values of 1.20, 5.14, and 14.81 μM, respectively. The compound induces apoptosis by upregulating Bax protein and downregulating Bcl-2 protein levels. Additionally, EGFR/COX-2-IN-1 significantly increases the proportion of cells in the G2/M phase in MCF-7 cells, demonstrating a broad-spectrum antitumor effect.</p>