Apoptosis

Zeluvalimab (AMG-404) is a monoclonal antibody designed to target the PD-1 receptor, and is utilized in cancer research [1].

Telitacicept (RC18), a fully human TACI-Fc fusion protein, acts as a dual inhibitor of B lymphocyte stimulator (BLyS) and APRIL (a proliferation-inducing ligand

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

Thalidomide-O-C6-NH2 is a synthesized E3 ligase ligand-linker conjugate used in the PROTAC dTAG-13, a degrader of FKBP12F36V and BET[1].

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

BcI-2/BcI-xI ligand 1, functioning as a BcI-2/BcI-xI ligand, is utilized in the synthesis of PROTAC BcI-2/BcI-xI Degrader-1 .

PROTAC GPX4 Degrader-1 (DC-2) is a PROTAC-based compound that efficiently degrades GPX4, demonstrating a degradation concentration (DC 50) of 0.03 μM in HT1080

2,2'-Dihydroxy chalcone inhibits β-glucuronidase (IC50=1.6 μM) and lysozyme (IC50=1.4 μM), and fights E. coli, S. fowleri, S. albicans, S. aureus.

Pyridinium bisretinoid A2E (A2E) is a fluorescent molecule isolated from the lipofuscin of retinal pigment epithelium, a weak photosensitizer.

Z-Asp-CH2-DCB is an irreversible inhibitor of broad spectrum caspase.

Anti-MousePD-1Antibody (D265A) is an antibody inhibitor targeting the PD-1 protein in mice.

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

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].

Sincalide ammonium, a CCK analog, stimulates bile release, gallbladder contraction, and sphincter relaxation, aiding in diagnoses.

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

Antiproliferative Agent-42 (Compound 7m), a dihydrodipyrrolo compound, exhibits antiproliferative activity against the Panc-1 cell line, with an IC 50 of 12.54

Lesigercept is a humanized antibody that targets IGHE.

RIPK2/3-IN-1 is a potent inhibitor of both RIPK2 and RIPK3 kinases, exhibiting IC50 values of 3 nM for RIPK2 and 117 nM for RIPK3.

Thalidomide-based E3 ligase ligand linked to a PROTAC piperazine-piperidine chain.

icFSP1 is a mitochondria-associated apoptosis-inducing factor regulator with antitumor activity for the study and treatment of tumor diseases.

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.

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.

YT117R is a PROTAC that targets degradation of FKBP12 and BRD4.

DAPK-IN-2: DAPK inhibitor with anticancer potential. Used in cerebral infarction and ischemia research.

Pipermethystine is a useful organic compound for research related to life sciences and the catalog number is T124340.

YL-5092, YTHDC1 inhibitor (IC50=7.4 nM), induces G0/G1 arrest and apoptosis, used for acute myeloid leukemia (AML).

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

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.

PARP1-IN-15 (Compound 6) is a PARP1 inhibitor that also inhibits tankyrase (TNKS) and promotes DNA double-strand breaks, leading to tumor cell apoptosis.

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

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%.

Ac-AAVALLPAVLLALLAP-LEHD-CHO is a caspase inhibitor targeting caspases 4, 5, and 9, demonstrating protective effects in MCF-7 cells treated with

ATPase-IN-3 is an ATPase (ATPase) inhibitor that can be used in the study of metabolism-related diseases.

S-(5'-Adenosyl)-L-methionine iodide, also known as S-Adenosyl-L-methionine iodide, is a vital methyl donor present in all living organisms [1].

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

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.

CPTH2 is an inhibitor of the HAT activity of Gcn5.

Thalidomide-5-propoxyethanamine acts as a cereblon (CRBN) ligand derived from Thalidomide, and it serves the purpose of recruiting the CRBN protein.

p53 and MDM2 proteins-interaction-inhibitor (racemic) is an inhibitor of the interaction between p53 and MDM2 proteins.

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.

Methyl-4-oxoretinoate is a synthetic retinoid with anticancer properties, used for skin conditions and potential ocular treatments.

PF-543 (Sphingosine Kinase 1 Inhibitor II), a novel sphingosine-competitive inhibitor of SphK1, inhibits SphK1 with IC50 and Ki of 2.0 nM and 3.6 nM.

Compound TPX-0046 is an inhibitor of RET. Compound TPX-0046 can inhibit the RET autophosphorylation. Compound TPX-0046 can be used for the research of cancer.

MY-943, a potent inhibitor of tubulin polymerization and LSD1, exhibits anticancer properties by inducing G2/M phase arrest, promoting apoptosis, and

3-Hydroxyterphenyllin from A. candidus is a fungal compound with antioxidant, anticancer, antibacterial, and antiviral effects.

PD-1/PD-L1 inhibitory peptide C8 disrupts the PD-1/PD-L1 interaction, leading to the activation of CD8+ and CD4+ T cells and an increase in IFN-γ secretion. In mouse models, PD-1/PD-L1 inhibitory peptide C8 has demonstrated antitumor activity.

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.

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

Satratoxin H is an air- and food-borne mycotoxin, which has been implicated in human health damage.

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.

Tubulin polymerization-IN-43 disrupts microtubules, arrests cell cycle, and induces apoptosis in leukemia by targeting colchicine sites.

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

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

FGFR1/VEGFR2-IN-3 (Compound 8m) acts as a dual inhibitor of FGFR1 and VEGFR2. This compound exhibits both anti-cancer cell proliferation and anti-migration activities, and it also has the capability to induce cell apoptosis (apoptosis).

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.

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.

Fludarabine triphosphate inhibits key enzymes, causing cell death.

SSE1806, a podophyllotoxin derivative (a natural antimitotic agent), functions as a microtubule/tubulin inhibitor, exhibiting potent anticancer and

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.

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

Thalidomide-5-PEG2-Cl is a cereblon ligand that recruits CRBN protein and forms PROTACs through linker conjugation.

PLD-IN-1 (Compound 3r) is an orally effective inhibitor of phospholipase D (phospholipaseD) with an IC50 of 1.97 μM. It reduces the expression of CD24, CD47, and PD-L1 while enhancing the expression of calreticulin, thereby modulating the immune evasion mechanisms of lung cancer cells by promoting the phagocytosis of cancer cells by macrophages. PLD-IN-1 inhibits the viability of lung cancer cell lines A549, HCC44, H460, and HCC15 with IC50 values of 18.44, 22.31, 24.85, and 21.45 μM, respectively. It induces apoptosis (apoptosis) in A549 cells and inhibits cell migration. Additionally, PLD-IN-1 increases pro-inflammatory M1 macrophage levels and decreases anti-inflammatory M2 macrophage levels, exhibiting anti-tumor activity in mouse models.

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

Annonacin is a cytotoxic acetogenin in Graviola leaf extract; it blocks mitochondrial complex and inhibits NKA/SERCA ATPase pumps.

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].

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

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.

CDK-TCIP1 is a bivalent molecule that links the CDK9 inhibitor SNS-032 with the BCL6 ligand BI3812. It effectively and specifically kills cells overexpressing BCL6, with an EC50 of 7.7 nM for SUDHL5 cells.

Compound 24a, an FPR1 antagonist, demonstrates potent inhibition of the formyl peptide receptor 1 (FPR1) with an IC50 value of 25 nM.

PROTACERα Degrader-9 (Compound 18c) is a dual-targeting PROTAC degrader designed to diminish estrogen receptor α (ERα) and aromatase (ARO). It demonstrates a Ki of 0.25 μM for ERα binding and an IC50 of 4.6 μM for ARO inhibition. This compound curbs proliferation in wild-type MCF-7 cells (IC50=0.54 μM) and ERα mutant variants MCF-7EGFR (IC50=0.075 μM), MCF-7D538G (IC50=0.31 μM), and MCF-7Y537S (IC50=2.3 μM), while also downregulating ERS1 and MYC expression. PROTACERα Degrader-9 arrests the cell cycle at the G2/M phase and induces apoptosis in MCF-7 cells, exhibiting antitumor efficacy in mouse models.

MS1943 is a orally bioavailable EZH2 selective degrader(IC50 of 120 nM).

MD-265 is a PROTAC degrader that targets and degrades MDM2, leading to the activation of p53 in cancer cells with wild-type p53. MD-265 achieves complete tumor regression and enhances long-term survival in leukemic mice.

Sarglaroids F (compound 6), an anti-inflammatory agent extracted from the roots of Grass Coral, suppresses LPS/ATP-induced IL-1β secretion by modulating K+

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

Cefatrizine inhibits eEF-2 kinase, affecting apoptosis, autophagy, and ER stress in cancers.

Tomatine hydrochloride halts fungi/bacteria growth, is extracted from wild tomato leaves, and precipitates steroids.

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

Ferroptosis-IN-12 (Cpd-A1) is an inhibitor of ferroptosis. It effectively suppresses ferroptosis in mouse renal tubular epithelial cells (mTECs) treated with Erastin and improves renal function in dose-dependent manners in mouse models of acute kidney injury (AKI) induced by ischemia/reperfusion (I/R) or cecal ligation and puncture (CLP). This compound also reduces renal tubular damage and eliminates inflammation. Exhibiting good plasma stability and high distribution in renal tissues during pharmacokinetic studies in mice, Ferroptosis-IN-12 shows promising potential for research in the field of AKI.

Diprovocim-1: TLR1/2 agonist; triggers TNF-α in THP-1 cells; boosts ovalbumin IgG1 & CTLs against tumors with anti-PD-L1 in mice.

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

Enniatin A1, a cyclic hexadepsipeptide from Fusarium, induces apoptosis and disrupts ERK, inhibiting ACAT (IC50: 49 μM).

PROTAC FLT-3 degrader 1 is a PROTAC FLT-3 degrader of internal tandem duplication (ITD)(IC50 0.6 nM),with anti-proliferative activity.

Bcl-2-IN-4: potent, selective, oral Bcl-2 inhibitor with 1.5 nM IC50, >200x selectivity over Bcl-xL.

ABBV-167 is a phosphate prodrug of the BCL-2 inhibitor venetoclax.

Pexelizumab is a humanized antibody targeting C5 to inhibit apoptosis and treat cerebral IR injury and myocardial infarction.

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

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.

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.

CDD-2807 is a serine/threonine kinase 33 (STK33) inhibitor with an IC50 of 9.2 nM. In mice, CDD-2807 demonstrates no significant toxicity and can cross the blood-testis barrier without accumulating in the brain. It offers reversible contraceptive effects, indicating potential for development as a male contraceptive.

AS-99 is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 μM, Kd= 0.89 μM) with anti-leukemic activity.

Suc-Ala-Leu-Pro-Phe-pNA (Suc-ALPF-pNA), a substrate for FK-506 binding protein (FKBP) [1], showcases the intricate interactions necessary for specific

Diethyl phthalate disrupts endocrine and induces apoptosis in PC12 cells; common in plastics, personal care items.

MDM2/4-p53-IN-3 inhibits MDM2/4-p53 PPIs (IC50: 18.5nM MDM2, 14.8nM MDM4), used in cancer research.

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.

ARV-393 HCl is an orally active and potent PROTAC targeting BCL6 with antitumor activity for the study of non-Hodgkin's lymphoma.

(R)-MIK665 is the less active enantiomer of MIK665. MIK665 is a special inhibitor of Mcl-1(IC50 of 1.81 nM).

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.

Anticanceragent 205 (compound 9) is an effective anticancer agent that binds to the G4-mtDNA target, inhibiting the replication, transcription, and translation of mtDNA (mitochondrial genome). It induces mitochondrial dysfunction, increases ROS production, and triggers DNA damage and cellular senescence. Anticanceragent 205 also promotes apoptosis and causes cell cycle arrest at the G0/G1 phase, showing potential for research in colorectal cancer.