Apoptose

PD-1/PD-L1-IN-39 (X 14) is an orally active PD-1/PD-L1 inhibitor with an IC50 value of 15.73 nM. It exhibits strong binding affinity to human and mouse PD-L1, with KD values of 14.62 and 392 nM, respectively. PD-1/PD-L1-IN-39 also demonstrates antitumor activity.

NAE-IN-1 (compound X-10) is a potent inhibitor of NAE1. It induces apoptosis and causes cell cycle arrest in the G2/M phase. Furthermore, NAE-IN-1 increases ROS levels and inhibits cell migration, demonstrating antiproliferative activity.

Ru-Poma is an Ru(II)-based photosensitizer designed to enhance the efficacy of photodynamic therapy (PDT) against tumors resistant to Cisplatin. It targets Pomalidomide to partially degrade CRBN, inducing ferroptosis by increasing lipid peroxides and downregulating GPX4 and GAPDH expression. In A549 cells, Ru-Poma exhibits cytotoxicity with IC50 values of 18.46 μM in the dark and 0.37 μM under illumination.

OPBP-1 is a D-peptide developed through phage display screening, molecular docking, and molecular dynamics simulations. It exhibits high stability, strong antitumor activity, and oral bioavailability. OPBP-1 selectively binds to the PD-L1 protein, significantly blocking the interaction between PD-1 and PD-L1, which helps restore and enhance T lymphocyte function while reducing the proportion of myeloid-derived suppressor cells (MDSCs), counteracting tumor-induced immune evasion. OPBP-1 is applicable for research in cancer immunotherapy.

RIP1 kinase inhibitor 9 (compound SY-1) is a selective inhibitor of RIP kinase. It effectively reduces central inflammatory responses caused by seizures. RIP1 kinase inhibitor 9 also obstructs Z-VAD-FMK-induced necroptosis in HT-29 cells, with an EC50 of 7.04 nM.

PROTACPD-L1 degrader-1 is a CRBN-based PD-L1-PROTAC degrader with significant PD-L1 protein degradation capacity. It demonstrates strong PD-L1 degradation activity in 4T1 cells, with a DC50 of 0.609 μM. This compound is applicable to breast cancer research.

Thalidomide-N-C3-O-C4-O-C3-OH is a conjugate of an E3 ligase ligand and a linker, used in the synthesis of the Aster-APROTAC degrader.

Apoptosisinducer 27 (compound 1c) is a potent inhibitor of MDA-MB-231 breast cancer cells, demonstrating an IC50 of 12.8 μM and inducing early apoptosis in these cells. Additionally, it can bind to DNA molecules as well as Bax and Bcl-2 proteins, thereby inducing DNA damage.

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!

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

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

4-hydroperoxy cyclophosphamide (4-OOH-CY) induces hepatotoxicity. It increases ghrelin levels and enhances inflammatory factors and oxidative markers.

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

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

YL5084 is a selective JNK2/3 inhibitor with IC50s: JNK2 (70 nM), JNK3 (84 nM), and antiproliferative, apoptosis-inducing effects.

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.

WF 10129 is a new angiotensin converting enzyme inhibitor generated by a fungus, Doratomyces putredinis.

FLT3-IN-29 (Compound MY-10) is an FLT3 inhibitor with IC50 values of 6.5 nM and 10.3 nM for FLT3-ITD and FLT3-D835Y mutants, respectively. It induces cell cycle arrest at the G0/G1 phase and effectively triggers apoptosis (Apoptosis). Additionally, FLT3-IN-29 reduces reactive oxygen species (ROS) and mitochondrial membrane potential (MMP), displaying anti-leukemic properties.

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

Thalidomide-derived cereblon ligand linked to a PROTAC technology linker, Thalidomide-O-amido-C3-NH2, is a synthetic E3 ligase ligand-linker.

Thalidomide-O-amido-C4-N3 (Cereblon Ligand-Linker Conjugates 4) is an E3 ligase ligand-linker conjugate incorporating the Thalidomide-based cereblon ligand and

C188, a naphthol-based STAT3 inhibitor, blocks IL-6-induced STAT3 activity in HepG2 cells, sparing STAT1.

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

MBC-11 trisodium, a bisphosphonate-Ara-C conjugate, may treat TIBD.

MYC-RIBOTAC, a ribonuclease-targeting chimera (RIBOTAC) specific to the MYC internal ribosome entry site (IRES), comprises an MYC mRNA-binding element tethered

ADAM-17 (TACE) and MMP inhibitor; attenuates TNF-α processing. Acts in concert with GM6001 to inhibit Chlamydia trachomatis growth.

Oxidosqualene cyclase inhibitor

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

Retifanlimab (MGA-012) is a monoclonal antibody targeting programmed cell death protein 1 (PD-1). Retifanlimab is used in studies of Merkel cell carcinoma.

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

FOXJ1 agonist 1 (compound 16c), an orally effective small molecule, effectively enhances FOXJ1 expression and acts on multiciliated cells (MCC) in the mammalian airway system to prevent chronic obstructive pulmonary disease (COPD). Foxj1-IN-1 induces motile cilia production in the respiratory system of both zebrafish and mammals and inhibits elastase-induced COPD in mouse models. Additionally, Foxj1-IN-1 demonstrates good liver microsomal stability and favorable in vivo pharmacokinetic (PK) curves and area under the curve (AUC). It exhibits negligible inhibition of CYP and hERG and lacks significant cytotoxicity.

Aloeresin G, a chromone glycoside isolated from Aloe, exhibits a moderate inhibitory effect on TNFα-induced NF-κB transcriptional activity, evidenced by an IC50

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

CPM-1285 induces apoptosis by effectively inhibiting the function of intracellular Bcl-2 and associated death antagonists.

(E/Z)-LAQ824 is an inhibitor of histone deacetylase.

Isorhamnetin 3-glucuronide is a useful organic compound for research related to life sciences and the catalog number is T124938.

Phosphocreatine dipotassium, primarily found in the skeletal muscles of vertebrates and one of organic compounds known as alpha amino acids and derivatives.

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

Thalidomide-O-amido-PEG3-C2-NH2 is a cereblon ligand-linker for PROTACs with a 3-unit PEG.

Sodium propionate (Propionic acid sodium salt) has potential anti-inflammatory and anti-apoptotic activities, inhibiting certain signaling pathways.

Silicon naphthalocyanine dichloride is a photosensitizer with potential anti-tumor activity. This compound is employed in photodynamic therapy to inhibit cancer by effectively absorbing specific wavelengths of light, thereby generating oxygen radicals that aid in the destruction of cancer cells. The biocompatibility of Silicon naphthalocyanine dichloride demonstrates promising prospects for medical applications.

MG-C-30 is an orally active CD27 agonist with an EC50 of 0.84 μM. It activates co-stimulatory signaling in NK cells and T cells, thereby enhancing the immune response. In the EG7-OVA mouse model, MG-C-30 demonstrates antitumor activity.

YJ1206 is a highly potent and selective CDK12/13 PROTAC degrader oral, DNA damage and cell-cycle arrest,and inhibits the proliferation of prostate cancer cells.

SC-2001 inhibits MCL-1 and STAT3, enhances SHP-1, induces apoptosis in breast cancer, and counters STAT3-driven sorafenib resistance in liver cancer.

Albicanol is a biochemical.

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

VEGFR-2-IN-68 (13b) is an inhibitor of VEGFR-2 with an IC50 value of 41.51 nM. It can induce apoptosis and cause G2/M cell cycle arrest, as well as exhibit anti-cancer metastasis properties.

Ceftiofur hydrochloride (U-67279A) is a stable, broad-spectrum 3rd-gen cephalosporin with antibacterial properties.

(E/Z)-10-Hydroxy-2-decenoic acid is a useful organic compound for research related to life sciences.

Streptonigrin, from Streptomyces flocculus, has anti-tumor and anti-bacterial properties, inhibiting PAD1-4.

Thalidomide-O-PEG4-NHS ester is a polyethylene glycol (PEG)-based linker, commonly employed for the synthesis of proteolysis-targeting chimeras (PROTACs)[1].

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

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

FD2157, a photosensitive PI3K inhibitor, exhibits inhibitory IC50 values of 43 nM for PI3Kα, 83 nM for PI3Kβ, 84 nM for PI3Kγ, and 14 nM for PI3Kδ.

WKYMVM is a N-formyl peptide receptor (FPR1) agonist.

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.

SF1126 is a first-in-class PI3K/BRD4 inhibitor and RGDS-conjugated LY294002 prodrug, enhancing solubility and targeting tumor integrins.

DRI-C21041 DIEA serves as an inhibitor of CD40/CD40L interaction, exhibiting an inhibitory concentration (IC50) of 0.31 μM.

Leucettamol A, from Leucetta microraphis, blocks LTB4 receptor and prevents Ubc13-Uev1A complex formation.

Emavusertib (CA-4948) hydrochloride, a selective and potent IRAK4/FLT3 inhibitor, is designed for oral administration. It achieves an IC 50 of 57 nM against IRAK4 in a FRET kinase assay and demonstrates anti-tumor activity [1] [2] [3].

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

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

DHFR-IN-23 (compound 5) is a dual inhibitor of DNA binders/DHFR, exhibiting an IC50 value of 0.08 μM against hDHFR. It serves as an apoptosis inducer and is applicable in research on ER+ breast cancer.

Tyroserleutide HCl, a tripeptide from pig spleen, inhibits tumor growth in vivo/vitro.

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.

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.

AVJ16 as a member of the insulin growth factor 2 mRNA-binding protein family, binds to the mRNA of certain genes to regulate protein translation.

Chloranil (tetrachloro-p-benzoquinone) induces inflammation and neurological dysfunction and can be used to model inflammation in mice.

Iparomlimab: anti-PD-1 IgG4κ antibody, targets PSB103 γ4/κ-chains, forms dimers, used in cancer research.

Nrf2 activator-9 (compound D-36) is an agent that mitigates oxidative stress by inhibiting the apoptosis of HUVEC cells induced by oxidized low-density

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.

Ecdysone is a major steroid hormone in insects and herbs.

HLDA-212 (Compound 43) is a bifunctional small molecule designed to target HaloTag-tagged protein (target protein, TP) and Aurora kinase A/B (AURKA/B, effector protein, EP). By binding TP and EP, it forms a stable ternary complex (TP:RIPTAC:EP) that inhibits the cell survival functions of EP, inducing apoptosis in cancer cells expressing TP. In 293_HFL cells, HLDA-212 demonstrates antiproliferative activity with a GI50 of 0.011 μM. This compound holds promise for treating cancers with high TP expression, such as prostate cancer and hematological malignancies.

(D)-PPA 1 TFA is a hydrolysis-resistant D-peptide antagonist and a potent PD-1/PD-L1 inhibitor, exhibiting an affinity for PD-1 of 0.51 μM and demonstrating

Pim-1 kinase inhibitor 4 is a potent Pim-1 kinase inhibitor with an IC50 value of 17.01 nM.Pim-1 kinase inhibitor 4 also possesses antioxidant activity and

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].

HDAC3-IN-2 (compound 4i), a pyrazinyl hydrazide-based HDAC3 inhibitor with an IC50 of 14 nM, effectively targets triple-negative breast cancer cells.

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

Human TNF alpha (46-65) peptide.

YTHDF2-IN-1 (Compound CK-75) is an inhibitor of YT521-B homology domain family 2 (YTHDF2) with a dissociation constant (Kd) of 26.2 μM, and it effectively blocks the interaction between YTHDF2 and m6A RNA. It suppresses colony formation in JAR cells and exhibits antiproliferative activity in various cancer cell lines, with an IC50 in the micromolar range. Additionally, YTHDF2-IN-1 induces apoptosis in K562 cells and causes cell cycle arrest at the G0/G1 phase.

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

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

TNF-α/IL-1β-IN-1 (compound 11a) is an anti-inflammatory agent that effectively reduces the expression of TNF-α and IL-1β, inhibits oxidative stress and myocardial cell apoptosis, and demonstrates significant activity against septic myocardial injury. Additionally, it improves myocardial blood flow in vivo.

BRD9 Ligand-5 (Compound 172-11) serves as a ligand for the target protein in PROTAC applications. It is utilized in the synthesis of CFT8634.

1D09C3 is a fully humanized anti-HLA-DR monoclonal antibody. It induces cell apoptosis (apoptosis) and death through a cascade of reactions, including reactive oxygen species (ROS) production, JNK activation, mitochondrial membrane depolarization, and the release of AIF from mitochondria. In xenograft models with JVM-2 cells and GRANTA-519 cells in mice, 1D09C3 demonstrated significant antitumor activity, improving overall survival and median survival time. This compound is applicable in cancer research, including studies on chronic lymphocytic leukemia (CLL).

C199 is a PROTAC degrader targeting PRMT4 with a DC50 of 106 nM. It demonstrates high selectivity for PRMT4 compared to other protein arginine methyltransferases. C199 exhibits strong cellular degradation capacity and induces apoptosis in multiple myeloma cell lines. It efficiently eliminates PRMT4 protein through the VHL-proteasome pathway. C199 has a relatively long half-life and shows potent anti-multiple myeloma (MM) activity.

Apoptolidin, from Nocardiopsis, induces apoptosis, targets mitochondrial ATPase (Ki 4-5 μM), kills glial cells, and has antibiotic and antifungal properties.

BRD4/FKBP12 degrader-1 (a1d) is an anticancer agent that functions as a BRD4/FKBP12 degrader.

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.

Compound 106 (compound 10ic) induces apoptosis in B16-F10 melanoma cells and potently inhibits metastatic nodules in mouse models of lung metastatic melanoma,

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

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

GLPG4970 is a potent, selective, orally active dual inhibitor of salt-inducible kinases 2 and 3 (SIK2/SIK3), with IC50 values of 0.3 nM and 0.7 nM, respectively. It exhibits weak inhibition of the hERG channel, with an IC50 value of 29 μM. GLPG4970 reduces the release of tumor necrosis factor α (TNFα) and increases the release of interleukin 10 (IL-10). This compound is applicable for research in inflammation and immunology, such as studies on colitis.