Apoptose

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

<p>Biotin-PEG6-Thalidomide is a PROTAC linker based on PEG.</p>

<p>VEGFR2/HDAC1-IN-1 (compound 13) is a potent dual inhibitor of VEGFR-2 and HDAC, with IC50 values of 57.83 nM for VEGFR-2 and 9.82 nM for HDAC.</p>

<p>HQY1428 is an orally active CDK12 inhibitor. It impedes DNA replication, causing cell cycle arrest at the G2/M phase in SKOV3 cells, and induces DNA double-strand breaks as well as apoptosis. In the SKOV3 xenograft mouse model, HQY1428 demonstrates antitumor activity. Additionally, when combined with the HER2 inhibitor Lapatinib in the NCI-N87 xenograft mouse model, HQY1428 produces a synergistic therapeutic effect.</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>"MRT-2359: Oral GSPT1 reducer, anti-cancer, targets NSCLC/SCLC, effective on MYC-driven cells."</p>

<p>Alkyl phosphates like (E)-C-HDMAPP activate γδ-T cells, resist hydrolysis, and boost TNF-α synthesis and γδ-T cell count in vivo.</p>

<p>FGFR1/VEGFR2-IN-2 (compound 6) is a dual inhibitor targeting both VEGFR2 and FGFR1 with IC50 values of 0.025 µM and 0.026 µM, respectively. This compound also exhibits inhibitory effects on EGFR and PDGFR-β, with IC50 values of 0.106 µM and 0.077 µM, respectively. FGFR1/VEGFR2-IN-2 demonstrates significant anticancer activity in the NCI-60 cell lines, showing a growth inhibition (GI) of 60.38%. In T-47D cell lines, it achieves an IC50 of 8.51 µM, exhibits anti-migratory properties, induces cell cycle arrest in the G1 phase, and promotes both apoptosis and necrosis. Additionally, while it has an IC50 greater than 100 µM in MCF-7 cell lines, it does so with an IC50 of 69.17 µM in MDA-MB-231 cell lines and shows no toxicity to normal cells.</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>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>Oxythiamine (Hydroxythiamin) is a TK inhibitor that inhibits cancer cell proliferation, induces cell cycle arrest, and induces apoptosis.</p>

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

<p>Poly(I:C) potassium is a synthetic RNA analog, activates TLR3/RIG-I, used as a vaccine adjuvant, and induces apoptosis in cancer cells.</p>

<p>Dapirolizumab is an anti-CD40 monoclonal antibody used in research on systemic lupus erythematosus (SLE) and other autoimmune diseases.</p>

<p>2-aminobenzo[d]thiazol-6-ol: antimicrobial, antioxidant, anticancer; may trigger cancer cell apoptosis.</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>MitoTam bromide hydrobromide is an electron transport chain (ETC) inhibitor.</p>

<p>LS-106 is an orally active, effective epidermal growth factor receptor (EGFR) inhibitor displaying antitumor activity both in vitro and in vivo. It inhibits the kinase activities of EGFR19del/T790M/C797S and EGFRL858R/T790M/C797S, with IC50 values of 2.4 nmol/L and 3.1 nmol/L, respectively, demonstrating stronger inhibition than Osimertinib. LS-106 induces cell apoptosis (Apoptosis), suppresses the proliferation of tumor cells carrying EGFR19del/T790M/C797S, and results in significant tumor reduction in a C797S mutant xenograft model.</p>

<p>c-Met/HDAC-IN-4, a dual inhibitor of c-Met/HDAC, exhibits an IC 50 value of 28.92 nM for c-Met. This compound effectively induces G 0 /G 1 phase cell cycle arrest and apoptosis in MDA-MB-231 breast cancer cells. Additionally, c-Met/HDAC-IN-4 suppresses both the proliferation and invasion of breast cancer cell lines.</p>

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

<p>QZ2135 (compound 20) is a PROTAC degrader that specifically targets RET and exhibits antitumor activity in vivo within a Ba/F3-KIF5B-RET-G810C xenograft mouse model. The compound demonstrates degradation activity with DC50 values of 4.7 nM (WT), 17.2 nM (V804M), and 73.8 nM (G810C) when targeting KIF5B-RET. QZ2135 is composed of the target protein ligand (red part) RETligand-3, the E3 ligase ligand (blue part) Lenalidomide-F, and the PROTAC Linker (black part) 7-Iodohept-1-yne, wherein the target protein ligand combined with the linker forms the conjugate RETLigand-Linker Conjugate-1.</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>F1324 acetate is an efficient, high-affinity b-cell lymphoma inhibitor with IC50 of 1 nM.</p>

<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>

<p>Pomalidomide-C5-Dovitinib (compound 2) is a PROTAC that links Pomalidomide and Dovitinib via a CRBN connector, exhibiting potent antiproliferative activity in</p>

<p>Thalidomide-O-PEG4-NHS ester is a polyethylene glycol (PEG)-based linker, commonly employed for the synthesis of proteolysis-targeting chimeras (PROTACs)[1].</p>

<p>CAY10678 is an mPGES-1 inhibitor that inhibits PD-1.CAY10678 reduces collagen deposition and T-cell depletion, and may be used to study melanoma.CASHIPS</p>

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

<p>CV-4-26 (Compound 22) acts as a covalent inhibitor of TEAD. By inhibiting YAP/TEAD-driven transcription, it diminishes the expression of CTGF and CYR61. Furthermore, CV-4-26 impedes colony formation in Huh7 and HepG2 cells, inducing cell cycle arrest and apoptosis (apoptosis). This compound demonstrates anti-tumoral activity against hepatocellular carcinoma (HCC) and hepatoblastoma (HB).</p>

<p>Bcl-2-IN-22 (compound 1), a gold (I) NHC complex, exhibits anticancer activity. It induces cell death (apoptosis) via the mitochondrial pathway with an IC50 value of 0.014 μM. Additionally, Bcl-2-IN-22 targets members of the BCL-2 family, promoting apoptosis and sensitization in multidrug-resistant leukemia cells overexpressing BCL-2.</p>

<p>Polyphyllin G (Polyphyllin VII), the the main member of polyphyllin family, shows strong anticancer activity against several carcinomas.</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>

<p>1,2-Naphthoquinone inhibits urease, induces apoptosis in PBMC cells, inhibitory activity against hiCE, hCE1, hAChE, and hBChE.</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>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>Mumefural, from Prunus mume fruit, hinders platelets, has anti-thrombotic properties, and boosts cognition.</p>

<p>DB818 dihydrochloride is the dihydrochloride salt form of DB818. It acts as an inhibitor of Homeobox A9 (HOXA9). By reducing the formation of the HOXA9-DNA complex, DB818 dihydrochloride inhibits the growth of AML cell lines OCI/AML3, MV4-11, and THP-1 and induces cell apoptosis (apoptosis).</p>

<p>FW-1 is a type I inhibitor of FLT3, with an IC50 of approximately 1 μM. It exhibits cytotoxic effects in FLT3-mutant AML cells, causes cell cycle arrest at the G0/G1 phase, and induces apoptosis in MV4-11 and MOLM-13 cells.</p>

<p>PROTAC Bcl2 degrader-1 is a PROTAC, which potently and selectively induces the degradation of Mcl-1 (IC50: 11.81 μM) and Bcl-2 (IC50: 4.94 μM; DC50: 3.0 μM).</p>

<p>PD-L1/VISTA-IN-2 (Compound S8) is an orally active dual inhibitor targeting PD-L1 and VISTA, with an IC50 of 1.4 μM for PD-L1 and a KD of 2.1 μM for VISTA. This compound can activate the tumor immune microenvironment, exerting anticancer effects.</p>

<p>Maceneolignan A, a natural product isolated from the aril of Myristica fragrans (Myristicaceae), inhibits β-hexosaminidase release in RBL-2H3 cells, exhibiting</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>DCZ3301 is a novel aryl-guanidino inhibitor.</p>

<p>Diethanolamine hydrochloride is HSD17B4 (hydroxysteroid 17-beta dehydrogenase 4) and pregnane X receptor (PXR), p53 Estrogen receptor.</p>

<p>Hypoxia inducer-1 (Compound N6) is a NO donor compound that is orally active and activated under hypoxic conditions. It exhibits high selectivity in releasing NO, inhibiting apoptosis, necrosis, and elevated levels of reactive oxygen species (ROS) associated with hypoxia. It modulates vasodilation and shows protective effects in a mouse model of myocardial hypoxic injury, making it useful for coronary heart disease research.</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>Ac-Pro-Gly-Pro-OH can be used as a CXCR2 agonist with bactericidal and anti-inflammatory activity for the study of sepsis and lung inflammation.</p>

<p>TOPOI/PARP-1-IN-2 (compound 6c) serves as a dual inhibitor targeting both PARP-1 and topoisomerase 1 (TOPO-1), with IC50 values of 32.2 nM and 46.2 nM, respectively. This compound exhibits greater selectivity for PARP-1 over PARP-2. Additionally, TOPOI/PARP-1-IN-2 disrupts the S phase of the cell cycle and induces apoptosis in the NCI-60 cancer cell lines.</p>

<p>Bfl-1-IN-5 (Compound (R,R,S)-26) is a selective inhibitor of Bfl-1, demonstrating an IC50 of 0.022 μM. This compound enhances the activity of caspase-3/7, with an EC50 of 0.37 μM, and also inhibits the viability of SU-DHL-1 cells, showing an EC50 of 1.3 μM.</p>

<p>Halenaquinone: PI3K inhibitor, stops RAD51 DNA binding &amp; osteoclastogenesis, induces PC12 cell apoptosis.</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>HSP90-IN-33 (compound 24e) is an effective Hsp90 inhibitor, demonstrating dissociation constants (Kd) of ≥200 µM for Hsp90α and 7.3 µM for Hsp90β. This compound induces cellular apoptosis (apoptosis) and arrests the cell cycle at the G0/G1 phase. Additionally, HSP90-IN-33 reduces the protein expression of ERα, CDK4, and Akt.</p>

<p>Ferumoxytol is an iron oxide nanoparticle with anti-leukemia properties, specifically against acute myeloid leukemia (AML) cells with low ferroportin (FPN) expression. By increasing intracellular iron levels, Ferumoxytol induces the Fenton reaction to produce reactive oxygen species (ROS), resulting in oxidative stress and ferroptosis. It selectively kills leukemia cells with low FPN expression while sparing normal cells, making it useful for studying leukemia targeting iron metabolism abnormalities.</p>

<p>CDK2-IN-32 (Compound 5g) is a selective CDK2 inhibitor with an IC50 of 0.21 μM. It exhibits cytotoxicity towards Vero cells with an IC50 of 28.52 μM.</p>

<p>FGFR1/VEGFR2-IN-3 (Compound 8m) acts as a dual inhibitor of FGFR1 and VEGFR2. This compound exhibits both anti-cancer cell proliferation and anti-migration activities, and it also has the capability to induce cell apoptosis (apoptosis).</p>

<p>LBM22, a CLK2 inhibitor, exhibits an IC50 value of 3.9 nM. It possesses anti-proliferative properties by inhibiting the phosphorylation of SR proteins. Additionally, LBM22 downregulates the expression of Wnt-related proteins and anti-apoptotic proteins, making it applicable in the study of non-small cell lung cancer.</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>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>Barakol, a primary compound found in Cassia siamea, inhibits MMP-3 activity and enhances the anti-metastatic effects of doxorubicin. Additionally, Barakol induces apoptosis (Apoptosis), generates reactive oxygen species, increases the Bax/Bcl-2 expression ratio, and activates caspase-9. This compound also exhibits laxative, anti-anxiety, central nervous system depressant, antioxidant, and anticancer properties.</p>

<p>Type-I/-II Photosensitizer-1 (compound 8b) is a photosensitizer with anticancer properties. It exhibits significant phototoxicity against A549 and 4T1 tumor cells. Under laser irradiation, Type-I/-II Photosensitizer-1 demonstrates strong oxygen-independent antitumor activity with an IC50 ranging from 1.50 to 1.76 μM.</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>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>KWCN-41, a RIPK1 inhibitor with 88 nM IC50, blocks necrosis, spares apoptosis, and is anti-inflammatory.</p>

<p>Lisaftoclax, an oral Bcl-2/Bcl-xl inhibitor (IC50: 2 nM &amp; 5.9 nM), treats CLL by promoting leukemia cell death.</p>

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

Bornyl acetate (Isobornyl acetate) has an anti-inflammatory effect. It is the volatile ingredient in some Chinese traditional herbs and numerous conifer oils.

<p>Thalidomide-based E3 ligase ligand-linker for PROTAC, with cereblon ligand and C8-NH2 hydrochloride.</p>

<p>Salinomycin sodium salt (Sodium salinomycin), an antibiotic potassium ionophore, is an effective inhibitor of Wnt/β-catenin signaling.</p>

<p>Sarglaroids F (compound 6), an anti-inflammatory agent extracted from the roots of Grass Coral, suppresses LPS/ATP-induced IL-1β secretion by modulating K+</p>

<p>AB-3PRGD2 is a radiolabeled agent that targets integrin αvβ3. It enhances tumor uptake and prolongs retention time in tumors, significantly improving the inhibition of tumor growth. AB-3PRGD2 also remodels the tumor immune microenvironment by upregulating PD-L1 expression and increasing tumor-infiltrating CD8+ T cells.</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>UM4118 (N-quinolin-8-ylpyridine-2-carboxamide) is a copper ion carrier used in the study of acute myeloid leukemia.</p>

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

<p>Src Inhibitor4 (Compound 18) is a derivative of KX-01 and functions as a Src inhibitor. It effectively disrupts tumor cells, damages microtubules, and induces cell cycle arrest, apoptosis, and immunogenic cell death. After introducing phenol or aniline functional groups, Src Inhibitor4 serves as a payload conjugation site for antibody-drug conjugates, showcasing antitumor activity.</p>

<p>CDK9-IN-36 (Compound T7) is a potent, selective, and metabolically stable CDK9 inhibitor with an IC50 value of 1.2 nM. It effectively suppresses the proliferation of Osimertinib-resistant NSCLC cells by downregulating Mcl-1, reducing colony formation, and inducing apoptosis. Additionally, CDK9-IN-36 exhibits antitumor activity in xenograft models.</p>

<p>UAMC-4821 is a ferroptosis inhibitor with an IC50 of 5.2 nM. It effectively scavenges free radicals, inhibits lipid peroxidation, and prevents ML162-induced ferroptosis, providing protective effects on HT-1080 cells. With favorable pharmacokinetic properties in mice, UAMC-4821 presents an oral bioavailability of 63% and demonstrates blood-brain barrier permeability.</p>

<p>Fluorescein-diisobutyrate-6-amide, a powerful inducer of ferroptosis, shows promise for cancer research applications [1].</p>

<p>Mitochondria modulator-2 (Compound Ir1) induces depolarization of the mitochondrial membrane potential, generates reactive oxygen species (ROS), inhibits the migration of A549 cells, causes cell cycle arrest at the G2/M phase, and triggers apoptosis in A549 cells.</p>

<p>EGFR-IN-143 (Compound 5f) is a potent EGFR inhibitor with an IC50 value of 0.15 μM. It induces apoptosis by arresting the cell cycle at the G2/M phase and exhibits antitumor activity.</p>

<p>MDM2ligand 4 is a ligand of MDM2 and can be used in the synthesis of the PROTAC degrader [KT-253].</p>

<p>Methylene Violet 3RAX is a cationic dye that is a potential photosensitizer in photodynamic therapy and has antitumor activity.</p>

<p>PQ401 (IGF-1R Inhibitor II) suppresses autophosphorylation of IGF-1R domain(IC50&lt;1 μM).</p>

<p>ReACp53 acetate could inhibit p53 amyloid formation and rescue p53 function in cancer cell lines.</p>

<p>TRK-IN-30 (Compound C11) is an inhibitor of tropomyosin receptor kinases (TRK), effectively inhibiting TRKA, TRKB, TRKC, and the resistant mutant TRKAG595R, with IC50 values of 1.8, 0.98, 3.8, and 54 nM, respectively. It also suppresses the activation of downstream PI3K/AKT and MEK/ERK signaling pathways. TRK-IN-30 hinders colony formation and cell migration of Km-12, induces cell cycle arrest at the G0/G1 phase, and triggers apoptosis in Km-12 cells.</p>

<p>Thalidomide-5,6-Cl is a cereblon ligand derivative that recruits CRBN protein and forms PROTACs with a linker.</p>

<p>TrxR-IN-7 (14f) is a potent inhibitor of thioredoxin reductase (TrxR), with an IC50 value of 3.5 µM. It exhibits antiproliferative activity and can induce apoptosis and the production of reactive oxygen species (ROS).</p>

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

<p>PROTAC 20S proteasome subunit β5 degrader 1 (compound 12f) serves as a targeted degrader of the 20S proteasome subunit β5, exhibiting a DC50 value of 0.11 μM in FaDu cells. This compound disrupts the cell cycle and promotes apoptosis (apoptosis), while inhibiting cell proliferation and migration in both FaDu and KM3/BTZ cells. It is applicable for research into resistance to Bortezomib in pharyngeal carcinoma and multiple myeloma.</p>

<p>PRLX-93936 HCL is an analog of erastin and demonstrated synergistic effects against non-small cell lung cancer (NSCLC) cells with cisplatin.</p>

<p>TRF2-IN-1 (compound F2) is a potent inhibitor of telomere repeat-binding factor 2 (TRF2). It exhibits antiproliferative activity and induces apoptosis. TRF2-IN-1 binds directly to the TRF2TRFH domain, selectively inhibiting TRF2 protein expression and telomere localization. Additionally, TRF2-IN-1 possesses anticancer properties and shows potential for osteosarcoma research.</p>

<p>NFh-NMe-2 is a photosensitizer that interacts with nitroreductase (nitroreductase) to generate singlet oxygen in tumor cells, exhibiting cytotoxicity in cancer cells and inducing apoptosis (apoptosis). In mouse models, NFh-NMe-2 demonstrates antitumor activity.</p>

<p>HDAC-IN-84 (compound 4a) is a potent HDAC inhibitor with IC50 values of 0.0045, 0.015, 0.013, 0.038, 5.8, and 26 μM for HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, and HDAC11, respectively. It effectively inhibits the proliferation of leukemia cells without causing toxicity.</p>

<p>PARP-1/2-IN-2-IN-1 (Compound 12e) effectively inhibits PARP1/2 and CDK12 with IC 50 values of 34 nM, 30 nM, and 285 nM respectively, impairing DNA damage repair</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>DefNEtTrp is an iron bis-chelating ligand composed of Def and Trp groups. It demonstrates potent broad-spectrum antiproliferative and cytotoxic effects in cancer cell lines. DefNEtTrp induces apoptosis and ferroptosis, exhibiting cytotoxicity with an IC50 value of 0.77 μM.</p>

<p>CDK4/6/HDAC-IN-1 (Compound N14) is a dual-target inhibitor of CDK4/6 and HDAC, with IC50 values of 7.23 nM for CDK4, 13.20 nM for CDK6, 55.66 nM for HDAC1, and 48.38 nM for HDAC6. It induces apoptosis and G0/G1 phase arrest through the HDAC-p21-CDK signaling pathway and can inhibit hepatocellular carcinoma.</p>

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

<p>BC13 is a CDK6/BRD4 inhibitor with IC50 values of 234 nM for CDK6 and 36 nM for BRD4. It exhibits antiproliferative properties, induces apoptosis (cell death) and DNA damage, and elevates ROS levels.</p>

<p>Thalidomide-O-PEG4-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].</p>