Apoptose

Pantoprazole Sodium Hydrate (BY1023 (sodium hydrate)) is a proton pump inhibitor drug, used for short-term treatment of erosion and ulceration of the esophagus

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

Pro-GA is a cell-permeable γ-glutamylcyclotransferase (γ-GGCT) inhibitor that inhibit proliferation in multiple bladder cancer cell lines. antitumour.

Petromurin C, a bis-indolyl benzenoid from P. muricatus, is cytotoxic to NS-1 cells (IC50=33μg/ml) and active against T. foetus (IC50=100μg/ml).

Finotonlimab (SCT-I10A), a humanized IgG PD-1 monoclonal antibody, shows potential in the research of solid tumors or lymphomas [1].

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.

Ac-AAVALLPAVLLALLAP-YVAD-CHO is a cell-permeable inhibitor of caspase-1 exhibiting antitumor activity [1].

MBC-11 trisodium, a bisphosphonate-Ara-C conjugate, may treat TIBD.

TAT-NEP1-40 TFA, a blood-brain barrier-permeable peptide, safeguards PC12 cells against oxygen and glucose deprivation (OGD) and fosters neurite outgrowth.

GPX4-IN-7 (Compound 31), an indirubin derivative, serves as a ferroptosis inducer in colon cancer treatment.

EMB-02 is a bispecific antibody targeting both PD-1 and LAG-3. It inhibits the downregulation of T cell activation and proliferation mediated by PD-1 and LAG-3, showing potent anti-cancer properties.

Taltirelin acetate (TA-0910 acetate) is a superagonist at thyrotropin-releasing hormone receptor (TRH-R)(IC50 of 910 nM and EC50 of 36 nM for stimulating an

Ferroptosis-IN-14 (compund 36) exhibits the most potent anti-ferroptotic activity with an EC50 value of 0.58 ± 0.02 μM, demonstrating excellent anti-ferroptotic efficacy, as well as stability in microsomes and plasma.

Z-VEID-FMK is a selective caspase-6 peptide inhibitor that irreversibly covalently binds to the enzyme, thereby inhibiting apoptosis and DNA breakage.

Avotaciclib hydrochloride, a CDK1 inhibitor, is the hydrochloride salt of Avotaciclib and exhibits potential therapeutic use in specific malignancies, including

RETligand-3 is the ligand for PROTAC QZ2135, which targets RET.

Beclin1-Bcl-2 Interaction Inhibitor 1 effectively disrupts the binding of Beclin 1 to Bcl-2, and is utilized in cancer and neurodegeneration research [1].

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.

Macrophage-activating lipopeptide 2 TFA (MALP-2 TFA) is a diacylglycerol lipopeptide and TLR-2/TLR-6 agonist activates immune cell responses macrophages,

Compound B12, a JOA derivative, collapses MMP to induce apoptosis, inhibits cloning/migration, and has an IC50 of 0.39 μM against HGC-27 cells.

EGFR-IN-78 (compound A5), a 2-aminopyrimidine derivative, serves as a reversible EGFR C797S-TK inhibitor and an apoptosis inducer.

Mcl-1 Inhibitor 15 (Compound (Ra)-15), with a K i of 0.02 nM, is utilized in cancer research [1].

LSD1-IN-24 is a selective and potent LSD1 inhibitor with an IC50 value of 0.247 μM.LSD1-IN-24 induces PD-L1 expression and enhances the T cell killing response

Tyroserleutide HCl, a tripeptide from pig spleen, inhibits tumor growth in vivo/vitro.

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

Ac-FEID-CMK TFA is a zebrafish GSDMEb-derived peptide inhibitor that acts by inhibiting the caspy2-mediated atypical inflammatory vesicle pathway.

PROTAC PD-1/PD-L1 degrader-1, a Cereblon-based inhibitor, blocks PD-1/PD-L1 with 39.2 nM IC50, boosting immune response and reducing PD-L1 via lysosomes.

IMMH 010 maleate (YPD-30 maleate) is a programmed cell death ligand 1 inhibitor used in the study of neurological disorders and advanced malignant solid tumors.

Chloranil (tetrachloro-p-benzoquinone) induces inflammation and neurological dysfunction and can be used to model inflammation in mice.

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

Ferroptosis-IN-3 (Compound 25), a ferroptosis inhibitor, demonstrates potent activity by inhibiting RSL3-induced ferroptosis in HT-1080 cells (EC50: 8.6 nM).

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

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

Asparanin A, an apoptosis inducer with anticancer properties, arrests the cell cycle in the G0/G1 phase via the mitochondria and PI3K/AKT signaling pathways.

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

Oral nitroimidazole antibiotic; treats anaerobic infections; may cause inflammation and muscle contractions with long-term use.

Lon-TK is a glycolysis inhibitor of LTB, linked with a linker conjugate. LTB is an intelligent responsive prodrug, comprised of Lonidamine (Lon) and a PD-L1 inhibitor (BMS-1), which are connected through a thioketal linkage. It effectively inhibits glycolytic metabolism in tumor cells and blocks the PD-1/PD-L1 immune escape pathway. Lon-TK holds potential for use in photodynamic-enhanced immunotherapy research.

2-Methylbiphenyl-oxadiazole-NH-Ph-CHO functions as a PD-L1 ligand for AUTACPD-L1degrader-3. It is also applicable in the synthesis of AUTAC.

Anticancer agent 130 (compound 8d) significantly induces apoptosis in A549 cells [1].

Pim-1 kinase inhibitor 4 is a potent Pim-1 kinase inhibitor with an IC50 value of 17.01 nM.Pim-1 kinase inhibitor 4 also possesses antioxidant activity and

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

PTD-p65-P1: a NF-kappaB inhibitor blocking activation from multiple inflammatory stimuli.

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

PD-1/PD-L1-IN-9, with an IC50 of 3.8 nM, is a potent and orally active inhibitor of the PD-1/PD-L1 interaction.

AZT triphosphate TFA, a Zidovudine metabolite, inhibits HIV & HBV replication and triggers mitochondrial apoptosis.

Collismycin A, from Streptomyces, has antibacterial, antiproliferative, and neuroprotective effects. It inhibits various cancer cells and is iron-complexing.

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

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.

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).

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].

GGTI298 trifluoroacetate (GGTI298TFA salt) is a geranylgeranyltransferase I inhibitor that causes cell cycle arrest and induces apoptosis.

BY13 is an SRC-3 PROTAC degrader with a DC50 of 0.031 μM. It selectively obstructs the ER signaling pathway by downregulating ERα levels, showing greater selectivity over the androgen receptor (AR). BY13 effectively addresses endocrine resistance in breast cancer by inducing cell cycle arrest at the G1 phase and triggering apoptosis. Additionally, it surpasses Fulvestrant in efficacy and significantly inhibits the growth of resistant breast tumors in LCC2 xenograft mouse models, exhibiting no noticeable toxicity.

Mcl-1 Inhibitor 12 (Example 10), with a K i of 0.22 nM, functions as an MCL-1 inhibitor. It is utilized in cancer research [1].

BRD9 Ligand-5 (Compound 172-11) serves as a ligand for the target protein in PROTAC applications. It is utilized in the synthesis of CFT8634.

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

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.

PROTACc-Met degrader-6 is a potent and orally active c-Met PROTAC degrader. It effectively promotes the degradation of c-Met protein, with DC50 values of 0.52 nM in EBC-1 cells and 0.45 nM in Hs746T cells. This compound almost completely abolishes the migration and invasion capabilities of tumor cells, significantly induces apoptosis (apoptosis), and arrests the cell cycle at the G0/G1 phase. PROTACc-Met degrader-6 is useful for studying various cancers, including non-small cell lung cancer and gastric cancer.

STAT3-IN-40 (Compound 8b) is an anticancer agent. It initiates immune responses in CD4+ and CD8+ T lymphocytes by inhibiting the expression and phosphorylation of STAT3, and induces ferroptosis and apoptosis in tumor cells. STAT3-IN-40 is valuable for research into cancer chemoimmunotherapy drugs.

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.

Apoptosisinducer 31 (compound 19) triggers caspase-dependent apoptosis (cell death). It plays a crucial role in cancer research.

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.

STK17A/B-IN-1 hydrochloride is a potent, selective, orally active inhibitor of STK17A/B, displaying an IC50 value of 23 nM against STK17A. It is utilized in the research of tumors.

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.

OBHSA（Oxabicycloheptane sulfonamide） is a novel selective estrogen receptor depressant (SERD) that can be used to study breast cancer.

SZU-B6, a PROTAC degrader, targets and degrades SIRT6 with DC50 values of 45 nM in SK-HEP-1 cells and 154 nM in Huh-7 cells. It inhibits the proliferation of SK-HEP-1 cells with an IC50 of 1.51 μM and suppresses colony formation in both SK-HEP-1 and Huh-7 cell lines. Additionally, SZU-B6 induces apoptosis in SK-HEP-1 cells and causes cell cycle arrest at the G2/M phase. It demonstrates anti-tumor activity in murine models.

KGYY15 (Mouse KGYY15), a peptide that targets CD40, exhibits weak inhibition of the CD40-CD40L interaction, with an IC50 exceeding 1 mM. At a concentration of 100 μM, KGYY15 activates the NF-κB pathway by 33%.

Bcl-2-IN-21 (compound C1), an iridium-based anticancer agent, effectively targets and inhibits Bcl-2, thereby impeding cancer cell colony formation and promoting increased levels of Bax and caspase 3.

Obestatin (human) is an endogenous ligand for G-protein eurythmic entity 39 formed by shearing of preproghrelin and can be used to study obesity.

JAK-IN-40 (Compound 46) is an inhibitor of JAK, effectively targeting JAK1, JAK2, and JAK3 with IC50 values of 0.022, 0.759, and 1.601 μM, respectively. It reduces the phosphorylation of STAT3 and inhibits the proliferation of cancer cells Ba/F3 and JAK1-TEL Ba/F3 with GI50 values of 0.614 μM and 0.193 μM. JAK-IN-40 arrests cell cycle progression at the G2/M phase in H1975 and H2087 cells, leading to apoptosis. Additionally, JAK-IN-40 exhibits a synergistic anti-tumor effect when used in combination with Osimertinib.

PROTACEGFRdegrader 14 is a potent and selective EGFR PROTAC degrader with a DC50 value of approximately 2.9 nM against EGFRL858R/T790M/C797S and a Dmax of 93.1%. It induces the selective degradation of EGFRC797S via a VHL and proteasome-dependent mechanism, downregulating EGFR-related transcriptomes. PROTACEGFRdegrader 14 exhibits high selectivity for EGFRWT, induces cell cycle arrest and apoptosis, and effectively inhibits tumor growth. It is applicable for research on non-small cell lung cancer (NSCLC).

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.

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.

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]

SZUH280 is a potent, selective PROTAC (proteolysis targeting chimera) HDAC8 (histone deacetylase 8) degrader, demonstrating a DC50 of 0.58 μM in A549 cells.

MEDI-7352 is a human bispecific antibody targeting NGF/bNGF and TNF. It can be utilized in research focused on osteoarthritis (OA) pain.

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

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.

Tat-ASIC1a (1-20) (mouse, rat) is a competitive ASIC1a transmembrane peptide with significant neuroprotective effects. It alleviates acidotoxic neuronal damage by targeting the ASIC1a-RIPK1 pathway and an auto-inhibition mechanism. This compound effectively safeguards the brain in ischemic stroke mouse models against damage from ischemia and is applicable in research on neurodegenerative diseases, such as Huntington's disease and Parkinson’s disease.

RET Ligand-Linker Conjugate-1 consists of a complex formed by a RET ligand and a linker, which can be utilized in the synthesis of QZ2135.

Necroptosis-IN-5 (Compound 26) is an orally active inhibitor of necroptotic cell death (necroptosis). This compound also exhibits potent inhibitory activity against receptor-interacting protein kinase 1 (RIPK1). It can be utilized in research related to inflammatory diseases, neurodegenerative disorders, and cancer associated with necroptosis.

5,10,15,20-Tetrakis(4-methoxyphenyl)porphyrin is a capable of forming complexes with metal ions and exhibit phototoxicity towards Hep-2 cells.

TopoisomeraseI inhibitor 17 (Compound 7h) is an inhibitor of TopoisomeraseI (Top1). It reduces DDX5 and reverses the locking effect of DDX5 on Top1 activity. This compound induces Top1-mediated DNA damage and promotes reactive oxygen species (ROS) production. It triggers apoptosis by decreasing anti-apoptotic proteins XIAP, Bcl-2, and Survivin, while increasing pro-apoptotic proteins Bax and γH2AX. Moreover, TopoisomeraseI inhibitor 17 halts progression at the G2/M checkpoint, leading to cell cycle arrest. It significantly impairs colorectal cancer cell colony formation and migration, and effectively reduces tumor size in human PDX tumor mouse models.

XY077 (compound 14a) is a RORγ inverse agonist with an IC50 value of 0.004 μM. It induces cell apoptosis (cellapoptosis) and exhibits antiproliferative activity both in vitro and in vivo.

Iron(III) compound induces ferroptosis in NB1 cells at 3μM, not apoptosis/necroptosis; inhibits various cancers, effective against drug-resistant NALM-6.

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.

EGFR/DHFR-IN-2 (9b) is a dual inhibitor of h-DHFR/EGFR TK, exhibiting IC50 values of 0.192 μM for h-DHFR and 0.109 μM for EGFR. It causes cell cycle arrest at the G1/S phase and induces apoptosis. Additionally, EGFR/DHFR-IN-2 (9b) is a potential inhibitor of CYP2C9 and CYP3A4. This compound can be utilized in cancer research.

Sec61-IN-4 (Compound 16b) is a potent Sec61 inhibitor with an IC50 value of 0.04 nM in U87-MG cells [1].

dASK1-VHL is an orally active PROTAC degrader targeting ASK1. It effectively binds to VHL, promoting the selective degradation of ASK1. By reducing ASK1 protein levels, dASK1-VHL inhibits the activation of p38 MAPK and decreases liver lipid content, offering new insights for MASH research.

SB-T-1214 (SBT) is a taxane-based drug known for its ability to effectively suppress the expression of stem cell-related genes (Oct4, Sox2, and c-Myc) and induce apoptosis in drug-resistant tumorigenic CD133+/CD44+ colon cancer spheroids. In Pgp+ DLD-1 human colon tumor xenograft mouse models, SB-T-1214 successfully inhibits tumor growth. This compound is relevant for anti-tumor research, particularly against drug-resistant tumors such as colon, pancreatic, and renal cancers.

Caspase-3/7 activator 1 is an effective activator of Caspase-3/7 that exhibits tumor-selective, antiproliferative activity and high apoptosis (Apoptosis) induction capability.

Thujopsene, a sesquiterpene found in T. dolabrata, exhibits a wide range of biological activities. It inhibits Na+/K+-ATPase and cytochrome P450 (CYP) isoform CYP2B6 with IC50 values of 25.9 µg/ml and Ki of 0.8 µM, respectively. Additionally, thujopsene demonstrates antimicrobial efficacy against both Gram-positive and Gram-negative bacteria, such as S. aureus, M. luteus, and S. typhimurium, with MICs ranging from 25-50 µg/ml. It also suppresses antigen-induced β-hexosaminidase release in IgE-sensitized RBL-2H3 mast cells (IC50= 25.1 µM) and shows cytotoxicity against A549 non-small cell lung cancer cells with an LC50 of 35.27 µg/ml. Furthermore, thujopsene causes mortality in mites D. farinae and T. putrescentiae, with LC50s of 9.82 and 10.92 µg/cm2, respectively.

PROTACPI3Kδ degrader-1 is a covalent PI3Kδ-targeting PROTAC degrader that targets lysine, with a DC50 of 3.98 nM. It exhibits potent antiproliferative activity and selective PI3Kδ inhibition (IC50: 8 nM). Additionally, PROTACPI3Kδ degrader-1 effectively degrades p-AKT, induces cell cycle arrest in the G1 phase, and promotes apoptosis and autophagy. It also significantly suppresses tumor growth in the SU-DHL-6 xenograft mouse model.

HMGB1-IN-2 (compound 15) is a selective inhibitor of the highly conserved nuclear protein HMGB1, demonstrating no inhibitory effect at an IC50 of 20.2 μM in

Thiocolchicine inhibits tubulin polymerization (IC50: 2.5 µM, Ki: 0.7 µM), induces apoptosis, and serves as an ADC cytotoxin.

Trimebutine (Mebutin) is a spasmolytic agent that regulates intestinal and colonic motility and relieves abdominal pain with antimuscarinic and weak mu-opioid