Apoptosis

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Product Citation
  1. TNF inhibitor

    Etanercept, a dimeric fusion protein that binds TNF, acts as a TNF inhibitor.
  2. SS28, a SRT501 analog with oral bioavailability, inhibits tubulin polymerization to cause cell cycle arrest at G2/M phase. SS28 results in apoptosis rather than necrosis tubulin.
  3. DCVC inhibits pathogen-stimulated TNF-α in human extra placental membranes in vitro.
  4. MDM2 inhibitor

    APG-115 (AA-115) is an orally active MDM2 protein inhibitor binding to MDM2 protein with IC50 and Ki values of 3.8 nM and 1 nM, respectively.
  5. dual MDM2/NFAT1 inhibitor

    MA242 is a dual inhibitor of murine double minute 2 (MDM2) and nuclear factor of activated T cells 1 (NFAT1) for Pancreatic Cancer Therapy.
  6. Bcl-2 Inhibitor

    Bcl-2 Inhibitor contains a mixture of two tautomers. A potent, cell-permeable, Bcl-2 inhibitor competes with Bak BH3 peptide for binding to Bcl-2 and Bcl-XL in vitro (IC50 =10 uM and 7 uM, respectively).
  7. MDM2/MDMX inhibitor

    WK23 is an inhibitor based on four aromatic groups and able to efficiently fill the binding pockets of MDM2/MDMX, its median inhibitory concentration (IC50) values to MDM2/MDMX are 1.17 and 36 uM, respectively
  8. RIP2 kinase inhibitor

    RIP2 kinase inhibitor 1 is a receptor interacting protein-2 (RIP2) kinase inhibitor extracted from patent WO/2014043446 A1, compound example 1.
  9. RIP2 kinase inhibitor

    RIP2 kinase inhibitor 2 is a receptor interacting protein-2 (RIP2) kinase inhibitor extracted from patent WO/2014043437 A1, compound example 9.
  10. Bcl-2 family inhibitor

    (+)-Apogossypol is a potent inhibitor of Bcl-2 family proteins; competing with the BH3 peptide-binding sites on Bcl-2, Bcl-XL, Mcl-1, Bcl-W, and Bcl-B, but not Bfl-1, with IC50s of 0.5 to 2 μM.
  11. Mcl-1 inhibitor

    AZD-5991 is a potent and selective Mcl-1 inhibitor with an IC50 of 0.7 nM in FRET assay and a Kd of 0.17 nM in surface plasmon resonance (SPR) assay.
  12. Bcl-XL inhibitor

    A-385358 is an inhibitor of Bcl-XL that enhances the in vitro cytotoxic activity of numerous chemotherapeutic agents (paclitaxel, etoposide, cisplatin, and doxorubicin) in several tumor cell lines.
  13. multi-targeted tyrosine kinase inhibitor

    Lenvatinib mesylate (E7080 mesylate), an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities.
  14. MCL-1 inhibitor

    AMG-176 is a potent, selective and orally bioavailable MCL-1 inhibitor, with a Ki of 0.13 nM.
  15. Mcl-1 inhibitor

    MIK665 (S-64315) is a special Mcl-1 inhibitor extracted from patent WO2016207225A1, compound Preparation 13, has an IC50 of 1.81 nM.
  16. Mcl-1 inhibitor

    Mcl1-IN-1 is a potent and selective inhibitor of the apoptosis regulating proteins Mcl-1.
  17. Mcl-1-PUMA interface inhibitor

    Mcl1-IN-8 (Comp8) is a Mcl-1-PUMA interface inhibitor, with a Ki of 0.3 μM. Mcl1-IN-8 (Comp8) exhibits dual activity on reduce PUMA-dependent apoptosis while deactivating Mcl-1-mediated anti-apoptosis in cancer cells.
  18. Mcl-1 Inhibitor

    Mcl1-IN-9 is a potent myeloid cell leukemia-1 (Mcl-1) Inhibitor with an IC50 of 446 nM in reengineered BCR-ABL+ B-ALL cells and a Ki of 0.03 nM.
  19. Mcl-1 inhibitor

    PROTAC Mcl1 degrader-1 (compound C3), a proteolysis targeting chimera (PROTAC), is a potently and selectively Mcl-1 inhibitor with an IC50 of 0.78 μM.
  20. BAD phosphorylat inhibitor

    NPB is a specific and potent inhibitor of BAD phosphorylation at Ser99, with an IC50 of 0.41 μM.
  21. Mcl-1 antagonist 1

    Mcl-1 antagonist 1 is a Mcl-1 protein antagonist extracted from patent WO2019173181, compound 200.
  22. Mcl-1 inhibitor

    Mcl1-IN-11 (Compound G) is a selective Mcl-1 inhibitor, less potent at Bcl-2, with Kis of 0.06 and 4.2 μM, respectively.
  23. MCL-1/PROTAC degrader

    dMCL1-2 is a potent and selective degrader of myeloid cell leukemia 1 (MCL1) based on PROTAC, which binds to MCL1 with a KD of 30 nM. dMCL1-2 activats the cellular apoptosis machinery by degradation of MCL1.
  24. Mcl-1 inhibitor

    Mcl1-IN-12 (Compound F) is a selective Mcl-1 inhibitor, less potent at Bcl-2, with Kis of 0.29 and 3.1 μM, respectively. Anti-tumor activity.
  25. insecticidal and anticancer

    Destruxin B, isolated from entomopathogenic fungus Metarhizium anisopliae, is one of the cyclodepsipeptides with insecticidal and anticancer activities. Destruxin B induces apoptosis via a Bcl-2 Family-dependent mitochondrial pathway in human nonsmall cell lung cancer cells.
  26. Bax agonist

    Bax-activator-106 is a specific Bax agonist. It acts by promoting Bax-dependent but not Bak-dependent apoptosis.
  27. DRAK2 inhibitor

    DRAK2-IN-1, compound 16, is a potent, selective and ATP-competitive DRAK2 inhibitor with IC50and Kivalues of 3 nM and 0.26 nM, respectively. DRAK2-IN-1 also has inbitory effect on DRAK1 (IC50=51 nM).
  28. OC2 inhibitor

    CSRM617 Hydrochloride is an inhibitor of the transcription factor ONECUT2 (OC2), thereby suppressing metastasis in mice.
  29. MDM2 inhibitor

    MI-1061 is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 potently activates p53, induces apoptosis, and has anti-tumor activity.
  30. RIPK3 inhibitor

    GSK-843 (GSK'843) is a receptor-interacting protein kinase 3 (RIP3 or RIPK3) inhibitor, which binds RIP3 kinase domain with an IC50 of 8.6 nM, and inhibits kinase activity with an IC50 of 6.5 nM.
  31. RIPK1 inhibitor

    PK68 is a potent and selective type II inhibitor of receptor-interacting kinase 1 (RIPK1) with an IC50 of ~90?nM, displays inhibition of RIPK1-dependent necroptosis.
  32. Lycopodine, a pharmacologically important bioactive component derived from Lycopodium clavatumspores, triggers apoptosis by modulating 5-lipoxygenase, and depolarizing mitochondrial membrane potential in refractory prostate cancer cells without modulating p53 activity. Lycopodine inhibits proliferation of HeLa cells through induction of apoptosis via caspase-3 activation.
  33. CD40-CD40L inhibitor

    DRI-C21045 is a potent and selective inhibitor of the CD40-CD40L costimulatory protein-protein interaction (PPI) with an IC50 of 0.17 ?M.
  34. MDM2/MDMX inhibitor

    RO-5963 is an inhibitor of the interaction of both MDM2 and MDMX with p53 with IC50s of ~17 nM and ~24 nM, respectively.
  35. MDM2 inhibitor

    PROTAC MDM2 Degrader-4 is a MDM2 degrader based on PROTAC technology. PROTAC MDM2 Degrader-4 composes of a potent MDM2 inhibitor, linker, and the MDM2 ligand for E3 ubiquitin ligase.
  36. MDM2 degrader

    PROTAC MDM2 Degrader-3 is a MDM2 degrader based on PROTAC technology. PROTAC MDM2 Degrader-3 composes of a potent MDM2 inhibitor, linker, and the MDM2 ligand for E3 ubiquitin ligase.
  37. MDM2 inhibitor

    PROTAC MDM2 Degrader-2 is a MDM2 degrader based on PROTAC technology. PROTAC MDM2 Degrader-2 composes of a potent MDM2 inhibitor, linker, and the MDM2 ligand for E3 ubiquitin ligase.
  38. MDM2 degrader

    PROTAC MDM2 Degrader-1 is a MDM2 degrader based on PROTAC technology. PROTAC MDM2 Degrader-1 composes of a potent MDM2 inhibitor, linker, and the MDM2 ligand for E3 ubiquitin ligase.
  39. Nutlin 3-based MDM2 ligand

    Nutlin carboxylic acid (MDM2 ligand 1) is the Nutlin 3-based MDM2 ligand. Nutlin carboxylic acid (MDM2 ligand 1) can be connected to the ligand for protein by a linker to form PROTACs.
  40. FTO inhibitor

    FB23-2 is a potent FTO inhibitor with an IC50 of 2.6 μM.
  41. Nutlin 3-based MDM2 ligand

    (4R,5S)-nutlin carboxylic acid (MDM2 ligand 2) is the Nutlin 3-based MDM2 ligand. (4R,5S)-nutlin carboxylic acid can be connected to the ligand for protein by a linker to form PROTACs.
  42. RIPK1 inhibitor

    RIPK1-IN-7 is a potent and selective RIPK1 inhibitor with a Kd of 4 nM and an enzymatic IC50 of 11 nM. RIPK1-IN-7 exhibits excellent antimetastasis activity in the experimental B16 melanoma lung metastasis model.
  43. Minnelide is a prodrug of triptolide that shows potent antitumor activity in a number of tumor types, particularly in pancreatic cancer. Minnelide causes apoptotic.
  44. Apoptosis inducer

    IV-23 (Compound 20) is a potent Noxa mediated apoptosis inducer, and it is a promising anticancer agent with potential. IV-23 inhibits cell growths in vitro and in vivo, reduces colony formation, arrests cell cycle at M phase, and induces esophageal squamous cell carcinoma (ESCC).
  45. RET inhibitor

    RET-IN-1 is a RET kinase inhibitor extracted from patent WO2018071447A1, Compound Example 552, has IC50s of 1 nM, 7 nM, and 101 nM for RET (WT), RET (V804M) , and RET (G810R), respectively .
  46. RIPK1 inhibitor

    RIPK1-IN-3 (Example 38), a RIPK1 inhibitor, extracted from patent WO2018148626A1, possesses anti-inflammatory proprieties.
  47. ETC inhibitor

    MitoTam bromide, hydrobromide is a tamoxifen derivative, an electron transport chain (ETC) inhibitor, spreduces mitochondrial membrane potential in senescent cells and affects mitochondrial morphology.
  48. Nitroaspirin (NCX 4016) is a nitric oxide (NO) donor and a nitro-derivative of Aspirin, which combines with Nitroaspirin to inhibit cyclooxygenase. Nitroaspirin (NCX 4016) has antithrombotic and anti-platelet properties and acts as a direct and irreversible inhibitor of COX-1.
  49. Lobaplatin (D-19466) is a diastereometric mixture of platinum(II) complexes. Lobaplatin (D-19466) shows activity for a variety of tumour types and is a promising antitumour chemotherapeutic agent.
  50. CAR agonist

    CITCO, an imidazothiazole derivative, is a selective Constitutive androstane receptor (CAR) agonist.

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