Apoptose

GPX4-IN-6 is a GPX4 inhibitor with antitumor activity.GPX4-IN-6 induces iron death and is used for the treatment and prevention of triple-negative breast cancer

Topoisomerase II inhibitor 14: powerful anticancer agent that induces apoptosis, halts S phase, and lowers GSH, MDA, and NO levels.

Tebentafusp (IMCgp100) is a protein that targets gp100 with potential anti-tumor activity.

Pitavastatin-d5 (sodium) is the deuterated form of Pitavastatin sodium. Pitavastatin (NK-104) sodium acts as a potent inhibitor of hydroxymethylglutaryl-CoA (HMG-CoA) reductase. In HepG2 cells, it inhibits cholesterol synthesis from acetate with an IC50 of 5.8 nM. Pitavastatin sodium is a highly effective inducer of hepatic low-density lipoprotein cholesterol (LDL-C) receptors.

CDK9-IN-24 (compound 21a) is a potent and selective inhibitor of CDK9 that exhibits a pronounced inhibitory impact on tumor proliferation.

ARB-272572 hydrochloride is a PD-L1 inhibitor that inhibits PD-1/PD-L1 cell signaling by inducing PD-L1 protein homology interactions.

Prodigiosin hydrochloride is a bioactive red pigment from bacteria with antibacterial, antifungal, anticancer properties, and inhibits Wnt/β-catenin.

Rapamycin is a potent and specific mTOR inhibitor that suppresses mTOR in HEK293 cells with an IC50 of 0.1 nM. It binds to FKBP12, thereby inhibiting mTORC1. Additionally, Rapamycin serves as an autophagy (autophagy) activator and functions as an immunosuppressant.

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.

ZYH-23 is a potent inhibitor of necroptosis. It targets HSP90 to inhibit the phosphorylation of RIPK1, RIPK3, and MLKL, effectively blocking programmed cell necrosis.

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.

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.

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.

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).

BCMA72-80: HLA-A2-specific peptide with high affinity; used in multiple myeloma and other BCMA+ tumor research.

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.

ZMF-24 is an anti-triple-negative breast cancer (TNBC) agent that exhibits IC50 values of 0.22 μM and 0.44 μM against BT-549 and MDA-MB-231 TNBC cell proliferation, respectively. It targets the eukaryotic translation initiation factor 3 subunit D (EIF3D), disrupting TNBC's energy supply by inhibiting glycolysis. Additionally, ZMF-24 induces TNBC cell apoptosis (apoptosis) by stimulating sustained endoplasmic reticulum stress.

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.

Diazepinomicin, from Micromonospora, blocks EGF-Ras-ERK pathway and induces apoptosis; an anti-tumor agent for K-Ras mutants.

PARP1/BRD4-IN-3 (compound HF4) is an effective inhibitor of BRD4 and PARP1, with IC50 values of 1210 nM and 2019 nM respectively. The compound exhibits antiproliferative activity, induces apoptosis (apoptosis) and cell cycle arrest at the G0/G1 phase. Additionally, PARP1/BRD4-IN-3 causes DNA damage and reduces the expression of the Rad51 protein, demonstrating anti-tumor activity.

Thalidomide-O-PEG4-amine is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

Citric acid-d4-1 is a deuterium-labeled variant of citric acid. Citric acid functions as a preservative and food additive. It induces apoptosis in HaCaT cells, causing cell cycle arrest at the G2/M and S phases. Additionally, citric acid leads to hepatic oxidative damage by reducing antioxidant enzyme activity and exhibits nephrotoxicity in mice.

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.

Cuprichydroxide exhibits inhibitory activity against Ralstonia solanacearum and A549 cells and has acute pulmonary toxicity.

L-threo-PPMP blocks GlcT, curbs glycosphingolipid creation, and triggers cell death, showing anti-cancer effects.

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.

Asunercept (APG101/CAN008) is a CD95-Fc protein targeting CD95L, used in GBM, MDS, and GvHD research.

RIPK1-IN-17 is a dual inhibitor of RIPK1 and RIPK3 inhibits necrosis by inhibiting phosphorylation of RIPK1, RIPK3 and MLKL,in a tnf-induced inflammation model.

Tubulin/AKT1-IN-1 (Compound D1-1) serves as an inhibitor of both tubulin polymerization and AKT pathway activation, effectively suppressing proliferation and

Anti-PD-L1/B7-H1 Antibody (29E.2A3) represents a chimeric antibody of mouse IgG2b, κ type, specifically targeting human PD-L1/B7-H1. The recommended isotype control for this antibody is Mouse IgG2b kappa, Isotype Control.

DEDN6526A (RG-7636) is a humanized ADC compound targeting endothelin B receptor (ETBR), which can be used to study melanoma.

Irofulven is an agent of DNA-damaging and antitumor. It is used for the treatment of advanced solid tumors, including prostate, ovarian, and pancreatic cancers.

Tanfanercept (HL036337) is an anti-TNF-α antibody, improving corneal erosions in dry eye mice.

Eriosematin has anti-proliferative and apoptosis-inducing properties and is a compound extracted from the root of Flemingia philippinensis in the Philippines.

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.

ROS inducer 5 (compound 6e) induces intracellular ROS accumulation and subsequent nuclear fragmentation. It can provoke apoptosis in MCF-7 cells with an IC50 of 3.85 μM. ROS inducer 5 is useful for cancer research applications.

Citatuzumab bogatox is a recombinant immunotoxin targeting EpCAM with the toxin bouganin, inducing apoptosis in EpCAM-positive tumors.

MitoTam bromide hydrobromide is an electron transport chain (ETC) inhibitor.

Tilogotamab (GEN-1029) is an agonistic hexameric complex targeting two independent epitopes on DR5, used for studying multiple myeloma (MM).

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].

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

Ropeginterferon alfa-2b (Ropeginterferon alfa-2b-njft), a monopegylated interferon-alpha (IFN-α), is utilized in the study of myeloproliferative neoplasms [1].

Tibulizumab (LY 3090106) is a bispecific antibody for BAFF & IL-17A; Kds: 60 & 14 pM; for autoimmune research.

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

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

RIP1-IN-1 is an orally bioavailable RIP1 inhibitor with a high binding affinity (Kd: 110 nM). This compound exhibits significant activity against necroptosis and effectively suppresses necrosome formation by inhibiting the phosphorylation of RIP1, RIP3, and MLKL pathways. RIP1-IN-1 can inhibit necroptosis and is applicable in research on acute liver injury.

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.

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.

Conjugated 18-C ω-6 fatty acid from Jacaranda seeds, induces cancer cell apoptosis via oxidative stress; metabolizes to cytotoxic CLA.

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

2-deoxy-D-Glucose-13C6 is an internal standard for GC/LC-MS, a glycolysis inhibitor, and induces apoptosis in certain cells at 2 mg/ml.

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

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.

MS78, an acetylation targeting chimera (AceTAC), specifically acetylates the p53Y220C mutant by recruiting the histone acetyltransferase p300/CBP.

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

[1,1'-Biphenyl]-3-amine is an inhibitor of MAO-A and MAO-B and can inhibit the cell viability of HT-29, HEK 293, and MCF-7 cells.

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%.

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

ADPM06: nonporphyrin PDT agent; leads in apoptosis, strong IC50 in µM against human tumors.

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

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.

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.

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

Amphiphilic peptide Mas7, a structural analogue of mastoparan is a known activator of heterotrimeric Gi-proteins and its downstream effectors.

PROTAC Mcl1 degrader-1 is a Cereblon ligand-based targeted chimeric protein degrader (PROTAC) and an Mcl-1 inhibitor, useful in cancer research.

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

AP1867-2-(carboxymethoxy), a moiety based on the synthetic FKBP12F36V-directed ligand AP1867, connects to the CRBN ligand through a linker to generate dTAG

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

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

ECDD-S18 (compound ECDD-S18) induces apoptosis in a dose-dependent manner, effectively targeting the vacuolar ATPase (V-ATPase) and impairing lysosomal acidification.

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

EGFR-IN-151 (Compound 10) inhibits EGFR and its downstream signaling pathways ERK/STAT3. It effectively suppresses the proliferation of various lung cancer cells, with IC50 values of 11.7, 5.19, 7.32, and 1.53 μM for NCI-H1781, HCC827, NCI-H3255, and NCI-H1975, respectively. Additionally, EGFR-IN-151 hinders colony formation and cell migration in H1975, induces G1 phase cell cycle arrest, and triggers apoptosis in H1975 cells.

Tubulin polymerization-IN-70 (compound Q19) is an effective inhibitor of tubulin polymerization. This compound exerts antiproliferative properties by targeting the colchicine binding site on tubulin, thereby inhibiting its polymerization. Tubulin polymerization-IN-70 also induces apoptosis and cell cycle arrest at the G2/M phase. Additionally, it triggers a decrease in mitochondrial membrane potential and elevates levels of reactive oxygen species (ROS). Moreover, Tubulin polymerization-IN-70 possesses anti-angiogenic and anticancer activities.

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.

Apoptosisinducer 30 (Compound 15a) acts as an anticancer agent. It induces apoptosis in MCF-7 cells through the mitochondrial pathway. This compound elevates intracellular levels of reactive oxygen species (ROS), decreases mitochondrial membrane potential, and arrests the cell cycle at the G0/G1 phase. Apoptosisinducer 30 inhibits cell growth, with an IC50 value of 0.32 μM against MCF-7 cells, and suppresses tumor growth in a mouse breast cancer model.

IC 86621: DNA-PK ATP-competitive inhibitor, IC50 120 nM, enhances DSB antitumor effects, EC50 68 µM for repair.

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.

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.

Ferroptosisinducer 6 (6d) is an inducer of ferroptosis (ferroptosis) that exhibits potent potential for Type I/II photodynamic therapy by inducing ROS production, oxidative stress, and mitochondrial damage. Additionally, it demonstrates antitumor activity.

ILS-920, a Rapamycin analog, has reduced immunosuppression, enhanced neuroprotection, and preferentially binds FKBP52 and L-type VGCC β1.

Asaretoclax is an effective inhibitor of B-cell lymphoma 2 (Bcl-2), demonstrating potential for use in cancer research.

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.

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.

DNMT-IN-4 (Compound 4d) is a DNMT inhibitor with an IC50 value of 5.78 µM. It induces apoptosis and exhibits anticancer activity.

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%.

Tubulin polymerization-IN-73 (Compound 37) is an inhibitor of microtubule polymerization with an IC50 of 1.8 μM. It induces cell cycle arrest at the G2/M phase and triggers apoptosis in A549 cells. The compound inhibits the proliferation of both A549 WT and A549/T resistant cells with IC50 values of 0.023 μM and 0.057 μM, respectively. Additionally, Tubulin polymerization-IN-73 demonstrates antitumor activity in mouse models.

Nemorosone, a PPAP from C. rosea, inhibits neuroblastoma and pancreatic cancer cell growth, induces apoptosis, and reduces mouse xenograft tumors.

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

Marstacimab (PF-06741086) is a neutralizing antibody that binds and inhibits human tissue factor pathway inhibitors.

MK-4166 is a humanized IgG1 agonistic monoclonal antibody targeting GITR. It is capable of enhancing the proliferation of both naive T lymphocytes and tumor-infiltrating T lymphocytes.

Tubulin polymerization-IN-45, a tubulin-targeting agent, acts as a tubulin polymerization inhibitor by binding to the tubulin's colchicine site.

Narasin (sodium salt) (HainanMycin) induces tumor necrosis factor-related apoptosis-induced ligand (TRAIL)-mediated apoptosis by ER stress in glioma cells and

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.

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.

Lacto-N-fucopentaose I is a milk oligosaccharide.

HDAC-IN-88 (Compound HJ-9) is a potent inhibitor of HDAC, effectively targeting HDAC6, HDAC1, HDAC2, HDAC8, and HDAC3 with IC50 values of 0.226, 1.103, 2.308, 3.255, and 3.864 μM, respectively. This compound suppresses the proliferation of cancer cells HepG2, HCT116, and MV4-11 with IC50 values of 5.47, 9.78, and 0.38 μM, respectively. Additionally, it inhibits the migration of HCT116 cells, causes cell cycle arrest at the G0/G1 phase, and induces apoptosis and autophagy in MV4-11 cells. HDAC-IN-88 reduces ROS levels and mitochondrial membrane potential and demonstrates antimalarial activity by inhibiting Plasmodium falciparum 3D7 with an EC50 of 165 nM. Furthermore, HDAC-IN-88 exhibits anti-angiogenic properties.

ReACp53 acetate could inhibit p53 amyloid formation and rescue p53 function in cancer cell lines.