Apoptosi

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

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

XmAb-2513 is a humanized monoclonal antibody inhibitor targeting CD30. It demonstrates significant anti-proliferative activity along with excellent antibody-dependent cellular cytotoxicity (ADCC) and antibody-dependent cellular phagocytosis (ADCP). XmAb-2513 is applicable in research on hematological malignancies such as Hodgkin lymphoma (HL) and anaplastic large cell lymphoma (ALCL).

SLF-amido-C2-COOH is a synthetic ligand for FKBP (SLF), and can be used in the synthesis of PROTACs.

LSD1-IN-27 inhibits LSD1 (IC50=13 nM), blocks gastric cancer cell stemness/migration, reduces PD-L1, and boosts T-cell response.

LP23, a non-arylmethylamine PD-1/PD-L1 inhibitor (IC 50: 16.7 nM), exhibits anti-tumor activity through the restoration of immune cell function in HepG2/Jurkat

PIYLGGVFQ is a TNF-α peptide inhibitor. It can suppress TNF-α-mediated apoptosis, nuclear translocation, and activation of NF-κB. In a CIA mouse model, PIYLGGVFQ has demonstrated anti-arthritic activity.

MK-1248 is a human IgG4 monoclonal antibody (mAb) targeting TNFSF18. It enhances the proliferative response of tumor-infiltrating lymphocytes to anti-CD3 stimulation and promotes the production of anti-tumor associated regulatory cytokines. MK-1248 is utilized in research on solid tumors.

2-Methylbiphenyl-oxadiazole-NH-Ph-NH-PEG3-C2-NH-Boc is the PD-L1 ligand-linker polymer of AUTACPD-L1degrader-3. It can be utilized in the synthesis of AUTAC.

NOD1-RIPK2-IN-1 (Compound 37) is an inhibitor of the NOD1-RIPK2 signaling pathway, displaying potent IC50 values of 42 nM and 1.52 nM against NOD1 and RIPK2, respectively. This compound effectively reduces the secretion of the pro-inflammatory cytokine IL-8, making it valuable for research in inflammation and immune disorders.

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.

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.

LTB is a prodrug formed through the conjugation of the glycolysis inhibitor (Lonidamine) and the PD1/PDL1 blocker (BMS-1) via a thioketal bond. LTB can encapsulate the photosensitizer Chlorin e6 (Ce6), constructing a co-delivery photodynamic nanoplatfform through self-assembly (LTB-6 NPs).

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

Compound LG-12, known chemically as PD-1/PD-L1-IN-50, is an inhibitor of PD-1/PD-L1. It enhances the secretion of IFN-γ, promotes the activation of CD8+ T cells, and activates T cell-mediated anti-tumor immunity.

Ac-VDQQD-pNA serves as a substrate for Caspase 2, which cleaves it to yield the yellow compound pNA (p-nitroaniline).

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.

RhoA-ROCK-IN-1 (Compound b19) is an inhibitor of the RhoA/ROCK pathway. It significantly inhibits cell proliferation, migration, and invasion, while promoting cell apoptosis (apoptosis). RhoA-ROCK-IN-1 exhibits strong anticancer activities by inhibiting the RhoA/ROCK pathway.

RIPK1-IN-27 (compound 19) is an inhibitor of RIPK1.

PMT-O9-1A is an effective PD-L1 degrader that reduces PD-L1 protein expression and exhibits cytotoxic properties. Additionally, PMT-O9-1A possesses anticancer activity.

IETD-CHO TFA (Caspase-8-IN-1) functions as a potent inhibitor of caspase-8 [1].

Ac-AAVALLPAVLLALLAP-LEVD-CHO is a cell-permeable inhibitor of caspase-4 that exhibits antitumor activity [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

TQB2916 is a humanized IgG2 monoclonal antibody agonist that targets CD40. It exhibits significant antitumor activity by occupying CD40 and activating immune function. TQB2916 is applicable for research in advanced solid tumors and lymphomas.

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

IBI356 is a humanized monoclonal antibody inhibitor that targets OX40L/CD134L/CD252. It can be utilized in the study of chronic inflammatory skin diseases, such as atopic dermatitis.

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.

PD-1/PD-L1-IN-52 (Compound Ⅲ-5) is an orally active inhibitor of PD-1/PD-L1 interaction, exhibiting an IC50 of 109.9 nM. It demonstrates antitumor activity in a C57BL/6 mouse model of MC38 colon carcinoma cells expressing human PD-1, achieving a tumor growth inhibition (TGI) rate of 49.6%.

PD-1/PD-L1-IN-51 (Compound III-4) is an inhibitor of PD-1/PD-L1 (IC50: hPD-L1 at 2.9 nM). It binds directly to PD-L1, blocking the interaction between PD-1 and PD-L1, and enhancing the release of IFN-γ. Additionally, PD-1/PD-L1-IN-51 exhibits antitumor activity.

Besufetamig is a bispecific antibody targeting programmed cell death protein 1 (PD-1) and the CD3ε chain. It modulates immune cell activity, exerting both immunosuppressive and antitumor effects. Besufetamig holds promise for cancer research.

Ac-DNLD-CHO (Ac-Asp-Asn-Leu-Asp-CHO) is an inhibitor of Caspase-3/7, exhibiting IC50 values of 9.89 nM and 245 nM, and approximate Ki values of 0.68 nM and 55.7

1,2-Naphthoquinone inhibits urease, induces apoptosis in PBMC cells, inhibitory activity against hiCE, hCE1, hAChE, and hBChE.

Lesigercept is a humanized antibody that targets IGHE.

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

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

Pegsunercept (PEG sTNF-RI), a pegylated monoclonal antibody, selectively binds to TNFA, incorporating a polyethylene glycol (pegol) moiety [1].

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

Onercept, a recombinant soluble form of the human tumor necrosis factor-alpha (TNF-α) p55 receptor, is utilized in the study of Crohn's disease [1].

Ranevetmab (NV-01), a caninized anti-NGF mAb, relieves pain in DJD research.

Atorolimumab (P3x22914G4), a monoclonal antibody, is employed in immunotherapies that target the programmed death-1 (PD-1) receptor [1].

Cofetuzumab (PF-06523435) is a antibody targeting protein tyrosine kinase 7 (PTK7), which can be used to synthesize ADC compounds like cofetuzumab pelidotin.

Anti-Mouse TNF alpha Antibody is a rat-derived IgG inhibitor targeting mouse TNF alpha.

Onfekafusp alfa (L19TNF), a trimeric fusion of L19 scFv and human TNF, targets malignant glioma.

Lorigerlimab (MGD019) is a bispecific IgG4 DART that blocks PD-1/CTLA-4, enhancing T-cells for mCRPC research.

Atibuclimab is a chimeric monoclonal antibody targeting CD14, consisting of a mouse variable region and a human IgG4 Fc region.

Lodapolimab (LY3300054) is an IgGλ anti- PD-1 monoclonal antibody [1] .

Anti-Mouse PD-L1/B7-H1 (LALA-PG) Antibody (10F.9G2) is an IgG2a, κ antibody inhibitor derived from mice, specifically targeting and inhibiting mouse PD-L1/B7-H1.

Anti-Mouse PD-1 Antibody (RMP1-14) is an IgG2a antibody inhibitor against mouse PD-1 and can block PD-1/PD-L1 signaling. High-Quality, Low-Cost!

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

δ-secretase inhibitor 11 is an inhibitor of δ-secretase and can be used as a lead compound for translational development of AD treatment.

Sotigalimab (APX 005) is a monoclonal antibody targeting CD40 with anticancer activity for the study of metastatic pancreatic cancer.

ACBI3 is a pan-KRAS degrader with anticancer activity, degrading oncogenic KRAS.

Sym029 is a human IgG monoclonal antibody (mAb) that targets TNFRSF5/CD40. It is applicable for cancer research. The suggested isotype control is Human IgG1 kappa, Isotype Control.

STAT3-D11-PROTAC-VHL (Compound D11-PROTAC) is a PROTAC degrader targeting signal transducer and activator of transcription 3 (STAT3). It demonstrates anti-tumor activity with IC50 values of 1335 nM in HeLa cells and 1973 nM in MCF-7 cells. The compound binds to the DNA binding domain of STAT3, recruits the E3 ligase VHL to form a ternary complex, leading to ubiquitination and subsequent proteasomal degradation of STAT3. Additionally, STAT3-D11-PROTAC-VHL inhibits tumor cell growth, induces cell cycle arrest and apoptosis (apoptosis), and suppresses tumor immune evasion.

ZS3-046 is a TAF1 PROTAC degrader that facilitates the ubiquitination and subsequent degradation of TAF1. It can activate p53 and induce apoptosis in acute myeloid leukemia (AML) cells. Additionally, ZS3-046 demonstrates anti-tumor efficacy in AML xenograft mouse models.

Anticanceragent 273 (Compound 9q) is an effective anticancer compound identified from matrine. It inhibits cancer cell proliferation, with an IC50 of 4.48 μM against HeLa cells. Anticanceragent 273 exerts its anticancer effects by modulating PI3K/AKT expression and activating activating transcription factor 4 (ATF4), which induces endoplasmic reticulum stress and triggers apoptosis. It holds potential for cancer research, including cervical cancer.

p38α inhibitor6 (compound 19) is a p38α inhibitor with an IC50 value of 0.68 μM. It induces apoptosis, arrests the cell cycle in the G0 and G2/M phases, reduces TNF-α concentration, upregulates the expression of the tumor suppressor gene p53, increases the Bax/BCL-2 ratio, and activates caspase3/7.

YCH3124 (compound Z33) is an inhibitor of USP7, exhibiting anti-tumor activity with an IC50 value of 41.9 nM. This compound demonstrates substantial in vitro anti-proliferative effects on various tumor cells, including LNCaP (IC50= 3.6 nM) and CHP-212 (IC50=9.9 nM). Moreover, YCH3124 induces apoptosis in CHP-212 cells by disrupting the cell cycle process during the G1 phase.

Photosensitizer-5, a photodynamic agent, exhibits cytotoxicity towards HeLa and HepG2 cells, with IC50 values of 10.4 nM and 6.9 nM, respectively. It induces cell death through lipid peroxidation via an iron-independent ferroptosis pathway. Additionally, Photosensitizer-5 displays antitumor activity in HeLa-tumor-bearing mice.

12-Deoxyphorbol 13-palmitate, a monomer derived from the roots of Euphorbia fischeriana, exhibits notable antitumor activity. This compound induces cell cycle arrest and apoptosis in gastric cancer cells by modulating key cell cycle regulators, such as cyclin B, cyclin A, and CDC2. Additionally, 12-Deoxyphorbol 13-palmitate significantly diminishes liver fibrosis by targeting APOL2 and impairing the APOL2–SERCA2–PERK–HES1 signaling pathway.

Ferroptosisinducer-4 (Compound 5) is a phospholipid-based ferroptosis inducer featuring a terminal double bond at the sn-2 position. It exhibits significant cytotoxicity towards HT-1080 cells with an IC50 value of 18 μM. The toxicity mechanism involves the generation of lipid peroxides and oxidative damage to the cell membrane induced by the terminal double bond. Ferroptosisinducer-4 can be utilized in studies pertaining to the regulation of ferroptosis.

Compound 7, also known as RAR/RXR agonist-1, is a chlorinated isomer of retinoic acid and acts as a selective RARα agonist and a partial RXRα agonist. It is capable of activating RXRα, thereby inducing G2/M arrest and apoptosis in cancer cells.

HNPMI is an epidermal growth factor receptor inhibitor that promotes apoptosis and is used in the study of colorectal cancer.

Anticancer Agent 153 (Compound 3) promotes apoptosis through the generation of Reactive Oxygen Species (ROS) and elevates the loss of Mitochondrial Membrane

Antiangiogenic agent 6 (Pt-1) effectively inhibits angiogenesis and induces necroptosis in tumor cells.

Antitumor Agent-103 (compound 24l) induces apoptosis and possesses antiproliferative and anti-colony formation properties.

Compound Rh1 (Anticancer agent 132) acts as an inducer of apoptosis and autophagy, exhibiting both antitumor and antimetastatic activities.

GSPT1 Degrader-1 (Compound 9q) effectively facilitates the degradation of G1 to S phase transition 1 (GSPT1) through the ubiquitin-proteasome system and induces

"TAT-BH4 (Bcl-xL) TFA, primarily localized at the mitochondria, inhibits apoptotic cell death.

Antitumor Agent-113 exhibits cytotoxicity in A549 cells, with an IC50 of 46.60 μM, and induces apoptosis, making it applicable for research in non-small cell

PROTAC FGFR2 degrader 1 (compound N5) is a potent PROTAC that efficiently targets FGFR2, boasting a DC 50 value of 6.46 nM and an FGFR2 IC 50 of 0.08 nM. This compound exhibits significant anti-proliferative effects and high selectivity. It induces G0/G1 arrest in the cell cycles of KATOIII and SNU16 and inhibits apoptosis by diminishing the activation of p-ERK and p-PLCγ, the downstream proteins of FGFR2. Additionally, PROTAC FGFR2 degrader 1 maintains over 50% inhibition of gastric cancer cells at a concentration of 0.17 nM and effectively suppresses the growth of SNU16 xenograft tumors in a mouse model.

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.

Apoptosisinducer 24 (Compound 4) inhibits the proliferation of gastric cancer cells with an IC50 range of 1.2-4.8 μM. It arrests the cell cycle at the G2/M phase, induces apoptosis in BGC-823 cells, and causes mitochondrial dysfunction. In mice, Apoptosisinducer 24 exhibits antitumor activity without significant toxicity, having an LD50 of 91.2 mg/kg.

TP4 (Nile tilapia piscidin) is an orally active piscidin-like antimicrobial peptide that exhibits inhibition of various gram-positive and negative bacterial

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

Antiproliferative Agent-27 (Compound 11) is a notable antiproliferative agent that markedly diminishes tumor cell colony formation and induces apoptosis,

Ferroptosis-IN-1, a diterpene derived from A.

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

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.

ZX782 acts as a GPX4 protein degrader and an inducer of ferroptosis (Ferroptosis), targeting GPX4 for destruction via both the ubiquitin-proteasome system and the autophagy-lysosome pathway. Following the degradation of GPX4 induced by ZX782, there is a significant increase in the accumulation of lipid reactive oxygen species (ROS) in HT1080 cells.

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

A-1248767, a derivative of A-1210477, is an MCL-1 inhibitor (IC50=23.9 nM; Ki=0.41 nM) known for its anticancer properties. It binds to MCL-1 with high affinity, induces an increase in MCL-1 protein levels inside cells, and promotes apoptosis in tumor cells.

Apoptosis Inducer 11 (compound 3u) promotes apoptosis via the mitochondrial pathway and elicits a G2/M block alongside a marked reduction in the S phase within

Ch282-5, an orally active inhibitor targeting the Bcl-2 protein, promotes mitochondria-dependent apoptosis (Apoptosis) by disrupting mitophagy and the mTOR pathway. It demonstrates antiproliferative effects on colorectal cancer cells, effective both in vitro and in vivo, while also inhibiting metastasis. Further, Ch282-5 augments Oxaliplatin-induced autophagy (Autophagy) by downregulating Mcl-1 protein and raising platelet count, which helps mitigate the adverse effects of Navitoclax.

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

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

Flaccidoside II, an active triterpenoid saponin from Anemone flaccida rhizome, both inhibits proliferation and induces apoptosis in Malignant Peripheral Nerve

Compound AuL9, also known as iNOS/TopoI-IN-1, is a multi-target hybrid molecule possessing anti-tumor, anti-inflammatory, and antioxidant properties. This compound effectively inhibits the growth of MCF-7 and MDA MB-231 breast cancer cells in vitro, exhibiting IC50 values of 3.5 μM and 6.3 μM respectively. It also prompts DNA damage and apoptosis in these cells by inhibiting human topoisomerase I (TopoI) with a K_i of 2.72 μM. Additionally, iNOS/TopoI-IN-1 reduces the expression of iNOS by suppressing the activation of NF-kB, with a K_i of 1.49 μM.

Compound Ru2 (Antitumor photosensitizer-6) exhibits synergistic type I/II photosensitization and photocatalytic activities under illumination at 595 nm. It causes oxidative redox imbalance within cells, affecting biosynthesis and metabolic processes, leading to cell apoptosis (Apoptosis). Compound Ru2 is applicable in studies of photodynamic therapy (PDT).

EGFRkinase inhibitor 7 (compound 18i) is an EGFR inhibitor with an IC50 of 42.3 nM, exhibiting anticancer properties. This compound demonstrates significant in vitro cytotoxicity and capacity to induce apoptosis. Furthermore, EGFRkinase inhibitor 7 displays anti-proliferative activity against human colon cancer cell line HCT116 and human non-small cell lung cancer cell line A549, with IC50 values of 4.82 µM and 1.43 µM, respectively.

H3R antagonist 4 (compound 11l) serves as a dual inhibitor of cholinesterases and histamine H3 receptors (H3R), demonstrating IC50 values of 7.04 μM (eeAChE), 9.73 μM (hAChE)(reversible), and 1.09 nM (H3R). It effectively inhibits both self and Cu2+-induced Aβ1-42 aggregation at 95.48% and 88.63%, respectively, and degrades Aβ1-42 protofibrils with 80.16% and 89.30% efficiency under similar conditions. Additionally, H3R antagonist 4 possesses the chelating capability for biometals Cu2+, Zn2+, Al3+, and Fe2+. It significantly reduces tau protein hyperphosphorylation induced by Aβ1-42, inhibits RSL-3 induced apoptosis and ferroptosis in PC12 cells, and shows optimal blood-brain barrier permeability and intestinal absorption characteristics in hCMEC/D3 and hPepT1-MDCK cells, respectively. Moreover, the compound improves learning and memory impairments in an Alzheimer's mouse model induced with scopolamine.

"Antitumor agent-96 (Compound D34) is a potent MRE11 inhibitor that down-regulates the homologous recombination (HR) pathway by binding to and suppressing the

BTK-IN-37 (compound 8d), a BTK inhibitor, demonstrates potent apoptotic effects on cancer cells by targeting BTK with K_i and IC_50 values of 5.07 nM and 3.6 nM, respectively. Additionally, this compound selectively promotes the enrichment of genes associated with necroptosis and pyroptosis.

Compound 2v (Anti-inflammatory agent 45) demonstrates anticancer properties with direct inhibitory impacts on the proliferation of various blood malignancies,

hCAIX/XII-IN-13 functions as an inhibitor targeting specific human carbonic anhydrases (hCA) IX and XII, crucial in tumor-related processes. Demonstrating efficacy, this compound offers inhibitory K i values of 0.08 µM for IX and 0.06 µM for XII. Additionally, under hypoxic conditions, hCAIX/XII-IN-13 enhances the effectiveness of Doxorubicin on MCF-7 cells by promoting G2/M phase cell cycle arrest and increasing apoptosis.

BAY 1892005 is a p53 protein modulator that targets the p53 condenser for the study of diseases associated with misfolded p53 protein

1-Methyl-1H-pyrrolo[2,3-b]pyridine exhibits cytotoxicity against MCF-7 cells and can be used in related research in the field of life sciences.

Anticancer Agent 146 (Compound 1.19) acts as a necroptosis inducer and demonstrates anti-tumor efficacy in the MDA-MB-231 mouse xenograft model [1].

RMC-4998 formic is an orally active inhibitor targeting the GTP-bound state of the KRASG12C mutant. It forms a trimeric complex with intracellular CYPA and the activated KRASG12C mutant, displaying an IC50 value of 28 nM. This compound inhibits ERK signaling and induces apoptosis in KRASG12C mutant cancer cells and is utilized in tumor research.