Apoptosis

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.

Secalonic acid D, from Aspergillus aculeatus, is anti-tumor, activates GSK3-β, degrades β-catenin, inhibits c-Myc, and induces apoptosis.

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

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.

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.

PROTAC EGFR degrader 6 effectively degrades EGFR Del19 in HCC827 cells (DC50=45.2 nM) and induces apoptosis and G1 arrest.

DH-18 is an inhibitor of matrix metalloproteinase-2 (MMP-2), exhibiting IC50 values of 139.45 nM for MMP-2, 518.11 nM for MMP-9, and 833.34 nM for MMP-8. The compound promotes cell apoptosis and causes cell cycle arrest in the G0/G1 phase. DH-18 also inhibits cell growth, making it potential for research in chronic myeloid leukemia.

CXCR4-IN-2 (compound A1), a potent bifunctional fluorinated small molecule, inhibits CXCR4 and exhibits anticancer properties by exerting cytotoxicity (IC 50:

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

MNK8 is a potent STAT3 inhibitor, impairs DNA binding, and inhibits liver cancer cell growth.

Anti-TNBC agent-8 (Compound TP2) is a photodynamic therapeutic compound that targets mitochondrial DNA G-quadruplexes (mtG4). Under white light exposure, it exhibits an IC50 of 0.42 μM against 4T1 cells. Anti-TNBC agent-8 tightly binds to mtG4, leading to the production of substantial reactive oxygen species (ROS) under illumination. This results in the loss of mitochondrial membrane potential (MMP), reduced ATP production, elevated ROS levels, and significant apoptosis in triple-negative breast cancer (TNBC) cells, thus demonstrating its tumor growth inhibitory activity. Anti-TNBC agent-8 is applicable for research in TNBC.

Tectorigenin sodium sulfonate, a derivative of tectorigenin, is synthesized through sulfonation with sulfuric acid followed by neutralization in saturated

PD-L1 ligand 1 is classified as a PROTAC-targeted protein ligand, primarily utilized as a degradation agent for PD-L1.

TNF-α-IN-9 is an NDM-1 inhibitor-3 analog and is a TNF-α inhibitor.TNF-α-IN-9 shows low inhibitory activity.

EGFR/COX-2-IN-1 is an EGFR/COX-2 inhibitor that effectively targets EGFRWT, EGFRT790M, COX-1, and COX-2 with IC50 values of 0.12, 0.076, 20.1, and 1.52 μM, respectively. It inhibits MCF-7, HT-29, and A-549 cells with IC50 values of 1.20, 5.14, and 14.81 μM, respectively. The compound induces apoptosis by upregulating Bax protein and downregulating Bcl-2 protein levels. Additionally, EGFR/COX-2-IN-1 significantly increases the proportion of cells in the G2/M phase in MCF-7 cells, demonstrating a broad-spectrum antitumor effect.

MK-0731 inhibits kinesin spindle protein, disrupting mitosis and triggering apoptosis in KSP-overexpressing tumor cells.

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

AZD1152 is a pro-drug of Barasertib (AZD1152)-hQPA. Which is a highly selective Aurora B inhibitor with IC50 of 0.37 nM in a cell-free assay.

Thalidomide-O-C2-acid: E3 ligase ligand-linker for PROTAC, with cereblon-derived Thalidomide component.

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.

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.

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

RD-23 is an orally active and selective RET PROTAC degrader. It facilitates the ubiquitination and degradation of the RETG810C mutant with a DC50 value of 11.7 nM. Additionally, RD-23 inhibits the activation of downstream Shc signaling and induces apoptosis (Apoptosis). It is useful for studying RET-related cancers.

HYS-072 is an orally active derivative of chrysin with antitumor properties. It induces apoptosis (Apoptosis) and autophagy (Autophagy) by inhibiting the PI3K/AKT/mTOR signaling pathway, and suppresses tumor growth in xenograft models in vivo by modulating autophagy-related pathways. HYS-072 is applicable for research in treating triple-negative breast cancer.

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.

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.

Milademetan tosylate hydrate, an oral MDM2 inhibitor targeting AML and solid tumors, induces G1 arrest and apoptosis.

Xerophilusin B from Isodon xerophilus halts ESCC cell growth, causes G2/M arrest, and induces apoptosis.

KRASG12C IN-16 (Compound SK-17) is a selective, covalent, and orally active KRASG12C inhibitor. It can induce apoptosis and effectively prevent the activation of the MAPK and PI3K/mTOR signaling pathways. Additionally, KRASG12C IN-16 exhibits antitumor activity against pancreatic cancer.

PKM2 modulator 1 (compound C998) is an effective PKM2 inhibitor with antiproliferative activity. It induces apoptosis and holds potential for research in glioblastoma studies.

Ac-AAVALLPAVLLALLAP-DEVD-CHO (DEVD-CHO-CPP 32) serves as a potent and reversible inhibitor of caspase-3 [1].

PZ703b hydrochloride, a Bcl-xl PROTAC, triggers apoptosis and halts cancer growth; used in bladder cancer studies.

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

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

Thalidomide-O-amido-C8-NH2 hydrochloride, a synthetic cereblon ligand-linker for PROTAC synthesis.

YX0798 is a selective, orally active CDK9 inhibitor (Kd: 0.28 nM). It downregulates the oncogenic protein c-MYC and the pro-survival protein MCL-1. YX0798 disrupts the cell cycle and causes transcriptome reprogramming, ultimately leading to apoptosis. The compound exhibits antitumor activity.

Lesigercept is a humanized antibody that targets IGHE.

EPZ020411 hydrochloride is a selective and potent small molecule PRMT6 inhibitor with an IC50 value of 10 nM.

Negative control for dTAGV-1.

Anticancer agent 52 exhibits potent cytotoxicity, induces apoptosis, and has potential in bladder cancer research.

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

CWI1-2 is a potent IGF2BP2 inhibitor that inhibits its interaction with M6A-modified target transcripts by binding IGF2BP2.

BRD6257 is an orally active inhibitor of protein phosphatase 1D (proteinphosphatase, Mg2+/Mn2+ dependent 1D, PPM1D) with an IC50 of 5 nM. It activates the p53 signaling pathway (EC50 of 51 nM), enhances p21 expression, and inhibits the proliferation of cancer cells MOLM13 (IC50 = 2.8 μM). BRD6257 demonstrates good metabolic stability in human and rat liver microsomes.

Stem bromelain: cysteine protease from pineapple stem with fibrinolytic, anti-inflammatory, antitumoral properties.

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.

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.

Balstilimab (AGEN2034) is a fully human monoclonal IgG4 antibody against PD-1 [1] .

Enlonstobart is a humanized IgG4-κ monoclonal antibody targeting PDCD1, functioning as both an immunostimulant and antineoplastic agent [1].

Rozibafusp alfa is an IgG2-κ antibody that targets ICOSLG, combined with a TNFSF13B fusion protein [1].

(R)-Q-VD-OPh is the less active enantiomer of Q-VD-OPha. Q-VD-OPha is an irreversible inhibitor of pan-caspase, with potent antiapoptotic properties.

Dehydrobruceine B, from Brucea javanica, enhances Cisplatin-induced apoptosis by affecting AIF, Bax, and Keap1-Nrf2.

Lenercept (Ro 45-2081) is a recombinant fusion protein combining the soluble TNF-receptor (p55) with the Fc portion of human IgG1 [1].

Latikafusp (AMG 256) is a fusion protein that is a PD-1 blocker and IL-21R agonist with antitumor activity.

PQ401 (IGF-1R Inhibitor II) suppresses autophosphorylation of IGF-1R domain(IC50<1 μM).

NF-κB-IN-19 (Compound 8) is an NF-κB inhibitor. It effectively induces DNA damage in tumor cells through the NF-κB signaling pathway and promotes the production of reactive oxygen species (ROS), as well as induces autophagy and apoptosis. Additionally, NF-κB-IN-19 inhibits levels of VEGF and HIF-1α, exerting antiproliferative effects in tumor cells through the PI3K/AKT and STAT-3 pathways. It is also effective in overcoming cisplatin resistance and exhibits antitumor activity.

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.

FLT3/HDAC-IN-1 is a dual inhibitor targeting FLT3 and HDAC, with IC50 values of 30.4 nM for FLT3 and 52.4, 14.7 nM for HDAC1/3, respectively. It induces apoptosis in MV-4-11 cells and exhibits antiproliferative effects against BaF3 cells transformed by FLT3 mutations. FLT3/HDAC-IN-1 is useful for research on refractory solid tumors and hematological malignancies.

Thalidomide-O-amido-PEG2-C2-NH2, which combines an E3 ligase ligand with a linker, serves as an immunomodulator for cancer treatment.

VEGFR-2-IN-53 (Compound 15w) is an inhibitor of VEGFR-2 with an IC50 value of 4.34 μM. It induces cell apoptosis (Apoptosis) and inhibits angiogenesis by blocking VEGFR-2 activity and preventing cell migration. Additionally, it shows an IC50 of 3.87 μM in inhibiting the growth of MCF-7 cells, making it pertinent for research in cancer therapeutics.

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

KSRP-IN-1 (compound 8) acts as an inhibitor of KSRP, inducing cell cycle arrest and apoptosis (Apoptosis). This compound demonstrates antitumor activity.

Canfosfamide, a prodrug activated by GSTP1-1, induces apoptosis and inhibits DNA-PK, producing an alkylating agent for cancer research.

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

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

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

HL435 is a heterobifunctional molecule that degrades BRD4 by linking with JQ1, with DC50 values of 11.9 nM and 21.9 nM in MDA-MB-231 and MCF-7 cells, respectively. It inhibits the proliferation of MDA-MB-231, MCF-7, 22Rv1, and A549 cells, arrests the cell cycle, and induces apoptosis. Additionally, HL435 exhibits antitumor activity in mouse models.

Sodium 2,4-dichlorophenoxyacetate: selective herbicide, controls broadleaf weeds by disrupting growth and protein/DNA synthesis.

Aspidin BB, a phloroglucinol from Dryopteris, inhibits cancer by causing cell cycle arrest and apoptosis in HO-8910 cells.

CDK9-Cyclin T1 PPI-IN-1 (Compound B19) is a selective inhibitor of the CDK9-Cyclin T1 protein-protein interaction (PPI), suppressing cell proliferation in TNBC

Gal-ARV-771 is a PROTAC prodrug, modified with galactose, based on ARV-771. It is activated in senescent cancer cells that express SA-β-Gal, thereby releasing ARV-771. Through the ubiquitin-proteasome pathway, Gal-ARV-771 induces selective degradation of the BRD4 protein in senescent cells and promotes apoptosis (apoptosis) of these cancer cells.

DC 81: Streptomyces-derived antitumor antibiotic, potent nucleic acid synthesis inhibitor, binds DNA sequences, forms covalent adducts.

JNK-1-IN-3 (Compound 9e) downregulates JNK1 and phosphorylated JNK1, reduces c-Jun and c-Fos expression in tumours, and restores p53 activity.

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

PUMA BH3 activates Bak, binds Bcl-2; triggers apoptosis via cytochrome C release; Kd 26 nM.

RET-IN-29 (Compound 8W) is a selective RET kinase inhibitor. It demonstrates inhibitory effects on BaF3 cells with the CCDC6-RETV804M mutation, with an IC50 of 0.715 μM. RET-IN-29 shows potential for research in non-small cell lung cancer (NSCLC).

Thalidomide-Piperazine 5-fluoride hydrochloride, a derivative of the cereblon (CRBN) inhibitor Thalidomide, serves as a ligand for E3 ubiquitin ligase (Ligands for E3 Ligase), facilitating the synthesis of PROTACs [1].

Thalidomide-O-C8-NH2 is a synthetic cereblon ligand & PROTAC linker, serving as an E3 ligase ligand-linker.

Anagrelide HCl monohydrate is a platelet-reducing imidazoquinazoline for ET and PV research.

SFI003 is a novel SRSF3 inhibitor that exerts anticancer activity against colorectal cancer by modulating the SRSF3 / DHCR24 / ROS axis and driving apoptosis in

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.

eIF4E-IN-2 effectively inhibits eIF4e, crucial for research on diseases like cancer.

AMG-7209 is an effective and selective MDM2-p53 interaction inhibitor.

DMUP inhibits CD47-SIRPα, induces apoptosis, boosts macrophage activity in A549 cells, and has antitumor properties.

22-SLF is a PROTAC degrader that operates by FBXO22-dependent degradation of FK506 Binding Protein 12 (FKBP12) with a DC50 of 0.5 µM. Additionally, 22-SLF can degrade other endogenous proteins, such as BRD4 and the EML4-ALK fusion protein (EML4-ALK fusion protein).

Compound PDK0379, with CAS No. 86-73-7, is a fragment molecule that serves as an important scaffold for molecular linking, expansion, and modification. Compound PDK0379 provides a structural basis and research tool for the design and screening of novel drug candidates, and is commonly used in drug discovery, drug synthesis, and related research.

BRAFV600E/JNK-IN-1 (Compound 14c) is an inhibitor of JNK1, JNK2, JNK3, and BRAFV600E, with IC50 values of 0.51 μM, 0.53 μM, 1.02 μM, and 0.009 μM, respectively. It also inhibits the phosphorylation of MEK1/2 and ERK1/2. Additionally, BRAFV600E/JNK-IN-1 suppresses tumor cell proliferation, NO release, and PGE2 production, exhibiting both antitumor and anti-inflammatory activities.

USP7-IN-9 is a potent USP7 inhibitor (IC50 = 40.8 nM), induces apoptosis, arrests RS4;11 cells, and modulates key oncoproteins.

Chloranthalactone B, a sesquiterpenoid from Sarcandra glabra, inhibits inflammation via AP-1 & p38 MAPK.

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

FB49 is a selective Bcl-2-associated athanogene 3 (BAG3) inhibitor with a Ki of 45 μM.

Carnitine palmitoyltransferase 2 (CPT2), an enzyme involved in fatty acid oxidation, serves as a prognostic biomarker for colorectal cancer (CRC).

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

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

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

NCT-58 is a potent HSP90 inhibitor that blocks Akt, downregulates HER family, and induces apoptosis in HER2+ breast cancer without triggering HSR.

Calcimycin (A-23187) is an antibiotic calcium ionophore that raises intracellular Ca2+ to induce cell death.

ZX703 is a protein hydrolysis-targeting chimera (PROTAC) that mediates the degradation of GPX4 through the ubiquitin-proteasome and autophagy-lysosome pathways, with a DC50 of 0.315 µM. It induces the accumulation of lipid reactive oxygen species (ROS), thereby promoting ferroptosis in cancer cells.

Euphjatrophane M (Compound 6) is a FOXO1 inhibitor that reduces NF-κBp65 phosphorylation and exhibits anti-inflammatory properties. It can inhibit the production of nitric oxide and also suppress the mRNA expression of IL-6, IL-1β, and TNFα in LPS-induced RAW 264.7 macrophages.

eIF4E-IN-6 (Compound 4b), a GMP analog, is designed to inhibit the eIF4E protein's ability to bind to cap mRNA.