Apoptosis

RIPK1ligand-Linker Conjugate-1 is a Target Protein Ligand-Linker Conjugate that consists of a RIPK1 ligand and a PROTAC linker, designed to recruit E3 ligase. It is utilized in the synthesis of PROTACRIPK1Degrader-1.

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

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

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].

(GalNAc)3-CPT is a glycan-conjugated prodrug that targets the asialoglycoprotein receptor (ASGR) overexpressed on liver cells. It demonstrates significant antitumor activity by activating the cGAS-STING pathway and promoting CD8+ T cell infiltration into tumor sites, leading to apoptosis of tumor cells. In HepG2 cells, it shows an IC50 value of 3.07 μM.

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

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

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

dPDL1-4 is a potent and selective eHSPTAC eHSP90PD-L1 degrader, with DC50 values of 7.77 μM (HeLa) and 6.52 μM (B16F10). It links eHSP90 to target proteins, inducing lysosomal degradation. dPDL1-4 effectively degrades PD-L1 and inhibits tumor growth, making it useful for research in cervical cancer and melanoma.

PI3Kδ-IN-25 is an orally active and selective PI3Kδ inhibitor with an IC50 of 2.1 nM. It exhibits IC50 values of 272, 285, and 1171 nM for PI3Kα, PI3Kγ, and PI3Kβ, respectively. In B16F10 cells, PI3Kδ-IN-25 inhibits the phosphorylation of AKTSer473, suppresses Treg cell proliferation, and downregulates the expression of PD-L1. In mouse models of B16F10 melanoma and Lewis lung cancer, PI3Kδ-IN-25 demonstrates anticancer activity by reducing tumor-infiltrating Treg cells and enhancing immune responses. This compound is applicable for research on cancers such as melanoma and lung cancer.

Ac-WEHD-AFC TFA: a fluorogenic substrate detecting caspase-1 activity, used in tumor and inflammation research.

VTX-0811 is a human IgG4 monoclonal antibody (mAb) that targets PSGL1/CD162. It modulates immune signaling pathways by enhancing TNF-α/NF-κB and chemokine-mediated signaling while reducing oxidative phosphorylation, fatty acid metabolism, and Myc signaling. VTX-0811 increases the proportion of CD8+ T cells among infiltrating T cells and exhibits antitumor activity in humanized mouse PDX models of melanoma.

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.

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

Ecdysone is a major steroid hormone in insects and herbs.

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).

CTP-347, a deuterated version of paroxetine, is potentially the best non-hormonal drug in its class for the treatment of hot flashes.

HPOB is an effective and specific HDAC6 inhibitor (IC50: 56 nM), >30-fold selectivity over other HDACs.

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.

Schisandronic acid is a triterpenoid acid isolated from the stems of Schisandra propinqua.

Zapalog: photocleavable dimerizer controlling instant protein interactions.

NS3694 is an inhibitor of apoptosis and inhibits apoptosome formation and caspase activation.

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.

Oenothein B inhibits PAR-glycohydrolase with antioxidant, anti-inflammatory, antifungal, anti-HCV, and antitumor effects.

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.

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.

Rasagiline (AGN1135) is an inhibitor of monamine oxidase used as adjunctive therapy in combination with levodopa and carbidopa in the management of Parkinsons

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

Human membrane-bound PD-L1 polypeptide serves as an antigen for inducing the production of PD-L1 antibodies [1].

HDAC-IN-77 (HL-5s), an HDAC inhibitor, has the capability to induce ferroptosis and suppress the Nrf2/HO-1 signaling pathway. This compound is utilized in cancer research.

Compound TE3, also known as ROS inducer 4, serves as a mitochondrial inhibitor. This compound induces a variety of mitochondria-related physiological alterations in tumors, including mitochondrial fragmentation, intense generation and accumulation of ROS, reduced mitochondrial membrane potential, and lower ATP content. Additionally, it activates ROS-mediated apoptotic signaling within mitochondria.

Enniatin complex: fungal cyclohexadepsipeptides inhibit enzymes, induce cancer cell apoptosis, and have ionophoric, antibiotic, and hypolipidemic effects.

RETligand-1 is a target protein ligand that specifically interacts with RET and can be utilized in the synthesis of the PROTAC LDD39.

Apoptosis Inducer 3 (Compound 3), a selective apoptosis triggering agent, induces both apoptosis and late-apoptosis phases, demonstrating cytotoxic effects

BGC4 is a gold(III) complex based on biphenyl. It inhibits human recombinant thioredoxin reductase (TrxR) with an IC50 of 10.7 μM, exhibits cytotoxicity with an IC50 of 5.4 μM in MDA-MB-231 cells, and induces apoptosis. Additionally, BGC4 demonstrates antitumor activity in mouse models.

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.

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.

LS-106 is an orally active, effective epidermal growth factor receptor (EGFR) inhibitor displaying antitumor activity both in vitro and in vivo. It inhibits the kinase activities of EGFR19del/T790M/C797S and EGFRL858R/T790M/C797S, with IC50 values of 2.4 nmol/L and 3.1 nmol/L, respectively, demonstrating stronger inhibition than Osimertinib. LS-106 induces cell apoptosis (Apoptosis), suppresses the proliferation of tumor cells carrying EGFR19del/T790M/C797S, and results in significant tumor reduction in a C797S mutant xenograft model.

Apoptosisinducer 26 (compound [AgCl(dap2SH)(PPh3)2]) is a mononuclear Ag(I) ligand-based autophagy inducer that exhibits antibacterial and anticancer activities against various bacterial strains and cancer cell lines. This compound facilitates the accumulation of Ag(I) ions in the periphery of bacteria, effectively inhibiting the growth of both Gram-positive (+) and Gram-negative (-) bacteria. Additionally, Apoptosisinducer 26 can intercalate between the base pairs of CT DNA, inducing apoptosis in A549 cells. It also possesses radical scavenging properties, which helps prevent oxidative stress.

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.

Destruxin B: cyclic peptide from Metarhizium fungus, induces apoptosis in lung cancer via mitochondrial pathway.

rac-CCT-250863 HCl: NEK 2 inhibitor, halts cell cycle, anti-cancer growth, boosts Pomalidomide-induced apoptosis.

Bfl-1-IN-6 (Compound 20) is an orally active inhibitor of Bcl-2-related protein A1 (BFL1) with an IC50 of 19 nM. This compound can stabilize BFL1 protein, activate cleaved caspase 3, and demonstrates antitumor activity in mouse models.

Bleomycin A5, or Pingyangmycin, is an oral glycopeptide antibiotic and acts as an antineoplastic and apoptosis inducer.

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

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.