Apoptosis

LSD1-IN-36, an effective LSD1 inhibitor with an IC50 value of 0.8 nM, induces cell apoptosis and arrests the cell cycle. This compound also exhibits antitumor activity.

<p>15-acetoxyscirpenol: ASM that induces apoptosis, inhibits Jurkat T cell growth dose-dependently, and activates caspases other than caspase-3.</p>

<p>CIGB-300 acetate (P15-Tat acetate) is a peptide that acts as an inhibitor of casein kinase 2 (CK2). It exhibits anticancer properties by disrupting the phosphorylation activity of CK2. CIGB-300 acetate induces apoptosis in various tumor cell lines and is applicable for cancer research.</p>

<p>β-Glucuronide-dPBD-PEG5-NH2 TFA is a β-glucuronide-linked pyrrolobenzodiazepine dimer employed in the synthesis of the antibody-drug conjugate (ADC) cIRCR201-</p>

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

<p>Anticancer Agent 102, a tetracaine derivative, exhibits anti-cancer activity by inducing apoptosis [1].</p>

<p>PIM-1/CK2-IN-2 (compound 3aA) is an inhibitor of the PIM-1/CK2 enzymes. This compound can induce the mitochondrial apoptosis pathway in CCRF-CEM cells and is utilized in cancer research.</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>HDAC6-IN-22 (compound 30), an HDAC6 inhibitor, exhibits an IC50 of 4.63 nM and demonstrates antiproliferative effects against multiple myeloma both in vitro and</p>

<p>VEGFR-2-IN-36 (compound 15) serves as a potent VEGFR-2 inhibitor, exhibiting an IC50 value of 0.067 μM, and acts as an apoptosis inducer with demonstrated</p>

<p>RMC-6291: Oral, covalent KRAS G12C inhibitor, blocks signaling, forms tri-complex with CypA, suppresses RAS activity in tumors.</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>Chetomin (BRN0077366) is an inhibitor of HIF-1 by weaken transcription of HIF-1, disrupting the binding of HIF-1α and HIF-2α to p300 at low nanomolar</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>TopoisomeraseIIα-IN-10 (Compound 13r) is a topoisomerase IIα inhibitor that binds to the active site of DNA when complexed with topoisomerase IIα. This binding is stabilized through interactions with DNA base pairs and amino acid residues. By intercalating into DNA, TopoisomeraseIIα-IN-10 induces apoptosis and disrupts the mitochondrial membrane potential in HCT116 cells, effectively inhibiting their growth with an IC50 of 4.37 μM. It is applicable for cancer research studies.</p>

<p>COG-1410 acetate is an apolipoprotein E-derived peptide and can be used in studies about neurological diseases.</p>

<p>TTQ-SA is a near-infrared spiraling aggregation-induced emitter capable of converting near-infrared light (NIR) into thermal energy, resulting in thermal damage and death of tumor cells. In cancer cells MF-7, TTQ-SA shows cell uptake and targeting capabilities. TTQ-SA binds with DNAzyme to inhibit the expression of the survivin gene, enhancing the sensitivity of tumor cells to photothermal therapy.</p>

<p>AFMK (Formyl-N-acetyl-5-methoxykynurenamine) is an active metabolite of Melatonin with antioxidant and free radical scavenging activity.</p>

<p>FB49 is a selective Bcl-2-associated athanogene 3 (BAG3) inhibitor with a Ki of 45 μM.</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>Mcl-1 inhibitor 3 shows good pharmacokinetic properties and excellent in vivo efficacy without toxicity.Mcl-1 inhibitor 3 is a highly potent and orally activate</p>

<p>cis-Clovamide is a naturally occurring phenolic compound with noteworthy antioxidant, anti-inflammatory, and antiapoptotic properties.</p>

<p>CQ627 is a molecular glue that targets the degradation of RIOK2. It effectively recruits the E3 ubiquitin ligase RNF126, inducing the proteasomal degradation of RIOK2 via the ubiquitin-proteasome system (UPS) in MOLT4 leukemia cell lines, with a DC50 value of 410 nM. Additionally, CQ627 induces apoptosis in a dose-dependent manner in these cells, blocking the cell cycle at the G2/M phase, and exhibits antiproliferative activity across various cancer cell lines. It also demonstrates in vivo anticancer activity in MOLT4 xenograft mouse models.</p>

<p>Theophyllol (theophylline sodium acetate) can alter calcium levels in subcellular fractions of rat brain cortex.</p>

XY221 (Compound 16o) selectively inhibits BRD4 BD2 with an IC50 of 5.8 nM. It demonstrates high selectivity for pan-BD2 and BRD4 BD2 domains, being 667 times more selective than for BRD4 BD1, and 9-32 times more selective than for BRD2/3/T BD2. XY221 can induce apoptosis in MV4-11 cells and exhibits anti-cancer activity.

<p>VEGFR-2-IN-61 (Compound 7b) is an inhibitor of VEGFR-2 with an IC50 of 2.83 µM. It effectively inhibits the proliferation of various cancer cells, including MCF-7 cells, with an IC50 of 2.12 µM. Additionally, VEGFR-2-IN-61 suppresses cell migration and induces oxidative stress and apoptosis in MCF-7 cells.</p>

<p>Compound A6, a potent PROTAC HDAC6 degrader, has a DC50 of 3.5 nM and induces apoptosis in myeloid leukemia cells.</p>

<p>Thalidomide-NH-C6-NH2 is a synthetic conjugate compound designed as an E3 ligase ligand-linker.</p>

<p>MS1943 is a orally bioavailable EZH2 selective degrader(IC50 of 120 nM).</p>

<p>GPLGIAGQ acetate: MMP2-cleavable peptide; stimulus-sensitive linker for MMP2-targeted liposomal/micellar carriers in photodynamic therapy.</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>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>Thalidomide-based E3 ligase ligand with PEG2-C2 linker; used as an immunomodulatory cancer treatment.</p>

<p>SDU-071 is a BRD4-p53 inhibitor, suppressing MDA-MB-231 cell proliferation, inducing cell cycle arrest and apoptosis.</p>

<p>PTD-p65-P1: a NF-kappaB inhibitor blocking activation from multiple inflammatory stimuli.</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>DP-15 acts as a degrader of GSPT1 and BRD4, with DC50 values of 5.25 nM and 0.48 nM, respectively. This compound exhibits antiproliferative activity in AML and NHL cells, showing IC50 values in the nanomolar range, induces G1 phase cell cycle arrest, and triggers apoptosis in MOLM13 cells. Additionally, DP-15 demonstrates anti-leukemic properties in the MOLM-13 xenograft mouse model. [Pink: ligand for target protein JQ-1 carboxylic acid; Black: linker; Blue: ligand for E3 ligaseCereblonThalidomide-5-OH]</p>

<p>84-B10 provides protection in cisplatin-induced acute kidney injury, reversing lipid peroxidation accumulation and downregulation of key ferroptosis inhibitors.</p>

<p>Dual Galectin-3/EGFR-IN-1 (Compound 29) is a dual inhibitor targeting Galectin-3 and EGFR, with dissociation constants (KD) of 52.29 μM and 3.31 μM, respectively. It inhibits TGF-β-induced hepatic stellate cell (HSC) activation, induces apoptosis in LX-2 cells, and shows antifibrotic activity in the liver.</p>

<p>EGFR-IN-144 (Compound 4B) inhibits EGFR (IC50=0.639 µg/mL) and tubulin polymerization (IC50=7.339 µg/mL). It exhibits cytotoxicity in various cancer cells with a GI50 at the nanomolar level. EGFR-IN-144 reduces the expression of mTOR, TNF-α, and IL-6, causes G1/S phase cell cycle arrest, and induces apoptosis.</p>

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

<p>FA4-Cu is a compound formed from the effective pancreatic cancer inhibitor FA4 and Cu(II), which can induce apoptosis by triggering ER and mitochondrial stress.</p>

<p>Anti-inflammatory agent 35 is a potent anti-inflammatory agent.</p>

<p>Citreoviridin from Penicillium citreoviride blocks brain Na+/K+-ATPase; boosts Na+/K+- and Mg2+-ATPase in microsomes dose-dependently.</p>

<p>This Bim peptide belongs to the pro-apoptotic group of the Bcl-2 family of proteins.</p>

<p>Caerin 1.1 TFA, a host defense peptide derived from the Australian tree frog Litoria's glandular secretions, exhibits anti-proliferative effects on HeLa cells</p>

<p>2'-Epi-2'-O-Acetylthevetin B (GHSC-74), a cardiac glycoside extractable from Cerbera manghas L.</p>

<p>Ara-SH, a derivative of Cytarabine with a mercaptopropionic acid substitution, serves as the initiator for the self-assembly of a smart, co-loaded Cytarabine</p>

<p>Pyridinium bisretinoid A2E (A2E) TFA, a fluorophore derived from retinal pigment epithelium (RPE) lipofuscin, initiates blue-light-induced apoptosis, mediates</p>

<p>MRIA9 inhibits SIK1/2/3 &amp; PAK2/3 with IC50: SIK1 (516 nM), SIK2 (180 nM), SIK3 (127 nM); ATP-competitive.</p>

<p>DD0-2363 (Compound 32d) is a dual-target inhibitor of WDR5-MLL1/HDAC. It can suppress the proliferation of acute myeloid leukemia cells and induce apoptosis. With its antitumor properties, DD0-2363 is applicable for research on acute myeloid leukemia.</p>

<p>Antitumor agent-112 (compound 3a) is a potent antitumor agent that induces apoptosis and exhibits cytotoxic activity on A549 cells, with an IC50 value of 91.35</p>

<p>NSD-IN-4 (Compound A8) is a potent and orally active inhibitor of NSD3, inducing apoptosis in a dose-dependent manner. It demonstrates significant antitumor activity against lung squamous cell carcinoma.</p>

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

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>Ganglioside GD3 disodium salt is a melanoma-associated antigen often targeted in immune therapy for melanomas.</p>

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

KTX-582: potent IRAK4/Ikaros degrader (DC50=4/5nM), induces MYD88 MT DLBCL apoptosis & tumor regression in lymphoma.

<p>PG-11047 2HCl treats genitourinary, immune, genetic, ocular, blood/lymphatic disorders, and aids lymphoma/prostate cancer research.</p>

<p>ERK1/2 inhibitor 13 (Compound 21y) is an orally bioavailable ERK inhibitor that targets ERK1 and ERK2, with IC50 values of 91.71 nM and 97.87 nM, respectively. It effectively suppresses the proliferation of cancer cell lines MCF-7, 4T1, MDA-MB-468, and HCC1970 with IC50 values of 0.67 μM, 2.76 μM, 2.15 μM, and 1.68 μM, respectively. Additionally, it inhibits cancer cell migration, induces apoptosis and autophagy in MCF-7 cells, and demonstrates anti-tumor and anti-metastatic effects in a 4T1 xenograft mouse model.</p>

<p>Negative control for dTAGV-1.</p>

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

<p>Thalidomide-O-amide-C5-NH2 is a synthetic E3 ligase linker combining cereblon ligand and PROTAC linker.</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>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>

Diethylnorspermine HCl (N1,N11-Diethylnorspermine tetrahydrochloride) potently induces SSAT (spermidine/spermine N1-acetyltransferase) mRNA and effectively

HX009 is a bispecific antibody that targets PD1 and CD47, though its binding to CD47 is attenuated. HX009 functions by blocking PD1/CD47 and can be utilized in research related to non-Hodgkin lymphoma (NHL).

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

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>Cathepsin B, a cysteine protease located within the subcellular endosomes and lysosomal compartments, mediates apoptosis and can be used in cancer research.</p>

<p>Tubulin polymerization-IN-72 (Compound 4a4) is a microtubule synthesis inhibitor with anticancer properties. By binding to the colchicine site, it disrupts the polymerization of tubulin, resulting in the arrest of cancer cells at the G2/M phase and inducing apoptosis (Apoptosis). The IC50 for its activity against cancer cells is 0.4-2.7 nM.</p>

<p>PD-1-IN-20 is the less active enantiomer of PD-1-IN-1.</p>

<p>Necroptosis-IN-3 (Cyclohexanecarboxamide, N-(2-thienylmethyl)-) (Compound 69) is a Necroptosis inhibitor that inhibits TNF-α induced necroptosis.</p>

SHP1 activator 1 (Compound 3n) is an activator of protein tyrosine phosphatase 1 containing the src homology-2 domain (SHP1), with an EC50 of 17.66 μM. It inhibits the proliferation of ABC-DLBCL cells and induces apoptosis by suppressing the STAT3 signaling pathway. In MDA-MB-231 cells, SHP1 activator 1 emits blue and green fluorescent signals, making it suitable as a cellular imaging agent.

Sodium valproate is an anti-epileptic, boosting brain GABA levels and possibly affecting potassium channels for membrane stability.

<p>Multi-kinase-IN-4 (compound 5d) is a multi-targeted kinase inhibitor active against VEGFR2, EGFR, HER2, and CDK2, with respective IC50 values of 0.33, 0.22, 0.</p>

<p>PDE4-IN-1 is a PDE4 inhibitor characterized by high potency (IC50: 8.6 nM) and superior selectivity over other PDE subtypes. This compound inhibits the release of inflammatory cytokines and chemokines. Additionally, PDE4-IN-1 significantly restores the damaged cAMP-CREB signaling pathway, inhibits proliferation, and promotes differentiation to reverse psoriasis formation.</p>

<p>Tubulin polymerization-IN-76 (compound 20b) is a potent and orally active inhibitor of tubulin polymerization. It acts at the colchicine binding site to inhibit tubulin polymerization with an IC50 value of 2.505 μM, effectively disrupting the intracellular microtubule network and interfering with mitosis. Tubulin polymerization-IN-76 shows significant inhibitory effects on MGC-803 and HGC-27 cells, with IC50 values of 1.61 and 1.82 nM, respectively. It effectively suppresses colony formation and cell migration activities in these cell lines, inducing G2/M phase cell cycle arrest and apoptosis (Apoptosis). Furthermore, Tubulin polymerization-IN-76 exhibits broad-spectrum antiproliferative activity.</p>

<p>Chol-CTPP targets the BBB and glioma cells; when combined with Chol-TPP, forms Lip-CTPP, enhancing anti-glioma drug efficacy.</p>

<p>MC-25B is a selective FKBP12 PROTAC degrader. It effectively degrades FKBP12 with a DC50 of 0.35 μM and a Dmax of 89%. MC-25B facilitates the degradation of nuclear-localized FKBP12 through a mechanism dependent on DCAF16.</p>

<p>BIO8898: potent CD40-CD154 inhibitor, IC50 of 25 µM, prevents CD40L-induced apoptosis.</p>

<p>ACBI3 is a pan-KRAS degrader with anticancer activity, degrading oncogenic KRAS.</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>TrxR1-IN-2 (Compound 6a) acts as a TrxR1 inhibitor that covalently bonds with the Cys475 and Sec498 sites of TrxR1. This interaction hampers TrxR1 activity, resulting in a redox homeostasis disruption and inducing apoptosis and ferroptosis.</p>

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

<p>Delmitide, a TNF-alpha production inhibitor, is used potentially for the treatment of Crohn's disease and ulcerative colitis.</p>

<p>TNF-α-IN-11 (Compound 10) is a TNF-α inhibitor exhibiting a dissociation constant (K D) of 12.06 μM.</p>

<p>Thevetiaflavone, a natural flavonoid from W. indica, blocks LDH leakage, boosting cell survival.</p>

<p>Inuviscolide induces apoptosis, G2/M arrest in melanoma, and has anti-cancer, anti-inflammatory effects.</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>Compound 29c, a Thalidomide-linker conjugate for potent PROTAC BRD2/BRD4 degrader-1, targets BET proteins.</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>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>Compound 13b, a potent EGFR degrader, inhibits and induces apoptosis in NSCLC cells with a DC50 of 13.2 nM.</p>

<p>Apoptosis inducer37 (Derivative 10) is an agent that induces apoptosis and exhibits anticancer properties by causing cell cycle arrest at the S-G2/M phase and promoting cell apoptosis. It significantly inhibits HCT116, SKOV3, and HepG2 cancer cells with IC50 values of 24.98 μM, 26.15 μM, and 23.09 μM, respectively. Apoptosis inducer37 demonstrates antitumor activity and can be utilized in ovarian cancer research.</p>

<p>EGFR/HER2/DHFR-IN-3 (compound 4c) serves as an efficacious dual inhibitor specifically targeting EGFR/HER2, exhibiting IC50 values of 0.138 μM for EGFR and 0.</p>

<p>TS-IN-6 (Compound 10) is a thymidylate synthase (TS) inhibitor with an IC50 value of 0.54 μM, showing significant antiproliferative activity. It can induce G1 phase cell cycle arrest and apoptosis (with notable increases in early and late apoptosis rates) and is useful for research in cancers such as colon, breast, and liver cancer.</p>

<p>Iparomlimab: anti-PD-1 IgG4κ antibody, targets PSB103 γ4/κ-chains, forms dimers, used in cancer research.</p>

<p>NMC-001 is a human IgG1 monoclonal antibody (mAb) that targets MDM2. It is useful for pancreatic cancer research. The recommended isotype control is HumanIgG1kappa, Isotype Control.</p>