Other inhibitors

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  1. TxA2 synthetase inhibitor

    CGS 15435, a potent thromboxane (TxA2) synthetase inhibitor with an IC50 of 1 nM, has a selectivity for Tx synthetase 100000-fold greater than that for cyclooxygenase, PGI2 synthetase and lipoxygenase enzymes.
  2. BTTAA is a Cu(I)-stabilizing ligand, whch performs potently with ubiquitin Glu18AzF.
  3. heparanase inhibitor

    Heparastatin is a heparanase inhibitor.
  4. MITF inhibitor

    ML329 is a micropthalmia-associated transcription factor (MITF) inhibitor, which inhibits TRPM-1 promoter activity with an IC50 of 1.2 μM.
  5. chymase inhibitor

    Chymase-IN-1 is a potent, selective, orally active, nonpeptide inhibitor of human mast cell chymase with an IC50 of 29 nM.
  6. REV7/REV3L interaction inhibitor

    REV7/REV3L-IN-1 is a REV7/REV3L interaction inhibitor with an IC50 of 78 μM.
  7. Cinperene is an atropine-like drug which can block pilocarpine-induced lacrimation and salivation.
  8. Y-9738 is a hypolipidemic agent.
  9. BMX kinase inhibitor

    CHMFL-BMX-078 is a highly potent and selective type II irreversible BMX kinase inhibitor with an IC50 of 11 nM.
  10. cholesterol-lowering agent

    TA-7552 is a potent cholesterol-lowering agent.
  11. PI5P4Kγ inhibitor

    NIH-12848 is a putative phosphatidylinositol 5-phosphate 4-kinase γ (PI5P4Kγ) inhibitor with an IC50 of 1 μM.
  12. bronchodilator

    Spirofylline is a bronchodilator, which can be used to treat asthma and bronchitis and emphysema.
  13. Rgp inhibitor

    Kgp-IN-1 is an arginine-specific gingipain (Rgp) inhibitor extracted from patent WO2017201322A1, compound 13-R.
  14. Eperisone is an antispastic agent used for treatment of diseases characterized by muscle stiffness and pain. Eperisone is a centrally acting muscle relaxant inhibiting the pain reflex pathway, having a vasodilator effect.
  15. TXNRD1 inhibitor

    TRi-1 is a potent, specific and irreversible inhibitor of cytosolic thioredoxin reductase 1 (TXNRD1), with an IC50 of 12 nM. TRi-1 has little mitochondrial toxicity for anticancer therapy.
  16. hydroxyethylamine based SPPL2a (Signal Peptide Peptidase Like 2a) inhibitor

    SPL-410 is an orally active, highly potent and selective hydroxyethylamine based SPPL2a (Signal Peptide Peptidase Like 2a) inhibitor, with an IC50 of 9 nM.
  17. TSPO ligand

    DPA-714 is a selective ligand for the translocator protein (TSPO) currently under evaluation for several clinical applications.It is also a PET tracer binding the TSPO receptor and highly expressed in myeloid cells.
  18. Zylofuramine is a psychomotor stimulant.
  19. ATAD5 inhibitor

    ML367 is a potent inhibitor of ATPase family AAA domain-containing protein 5 (ATAD5) stabilization, acts as a probe molecule that has low micromolar inhibitory activity. ML367 blocks DNA repair pathways, suppresses general DNA damage responses including RPA32-phosphorylation and CHK1-phosphorylation in response to UV irradiation.
  20. BPK-29 is a specific ligand that disrupts the atypical orphan nuclear receptor NR0B1-protein (such RBM45 and SNW1) interactions by covalently modifying C274. BPK-29 impairs the anchorage-independent growth of KEAP1-mutant cancer cells.
  21. bumped kinase inhibitor

    BKI-1369 is a bumped kinase inhibitor (BKI). BKI-1369 increases human Ether-a-go-go-related gene (hERG)-inhibitory activity with an IC50 of 1.52 μM.
  22. Dicyclanil is an insect growth regulator compound with a similar chemical structure to cyromazine.
  23. D5D inhibitor

    D5D-IN-326 is a selective, orally active delta-5 desaturase (D5D) inhibitor, with IC50s of 72 and 22 nM for rat and human D5D in enzymic and cell-based assays, respectively, has no effect on D6D or D9D activity.
  24. AKOS B018304 is an arylalkylidene derivative, with polar substitution at para-position.
  25. SMS2 inhibitor

    Ly93 is a selective and oral active sphingomyelin synthase 2 (SMS2) inhibitor, with an IC50 of 91 nM.
  26. NAAA inhibitor

    ARN 077 is a potent and selective N-acylethanolamine acid amidase (NAAA) inhibitor with an IC50 of 7 nM for human NAAA. ARN 077 significantly increases palmitoyl ethanolamine (PEA) levels within the CNS and has broad antinociceptive activity in mice and rats.
  27. (S)-Metolachor, a derivative of aniline, is a major pesticide in use.
  28. metabolite of TA-0910

    TA 0910 acid-type is a metabolite of TA-0910.
  29. Malat1 inhibitor

    MALAT1-IN-1 is a potent and specific Malat1 (Metastasis-associated lung adenocarcinoma transcript 1) inhibitor.
  30. Propionylcarnitine is a propionyl ester of L-carnitine.
  31. Eprodisate is a new compound designed to interfere with interactions between amyloidogenic proteins and glycosaminoglycans and thereby inhibit polymerization of amyloid fibrils and deposition of the fibrils in tissues.
  32. OGA inhibitor

    MK-8719 is a highly potent and selective OGA inhibitor (EC50 = 52.7 nM) which is a Potential Treatment for Tauopathies. MK-8719 showed excellent CNS penetration that has been advanced to first-in-human phase I clinical trials.
  33. Methyl β-D-glucopyranoside is used to synthesize natural glycophenolics via enzymatic caffeoylation.
  34. LYPLAL1 inhibitor

    LYPLAL1-IN-1 (Compound 11) is an selective covalent small-molecule inhibitor of Lysophospholipase-like 1 (LYPLAL1) with an IC50 of 0.006 μM. LYPLAL1-IN-1 increases glucose production.
  35. SET domain inhibitor

    MMSET-IN-1 is a multiple myeloma SET domain (MMSET, aka NSD2/WHSC1) inhibitor against SETD2 and MMSET with IC50s of 0.49 and 3.3 μM, respectively. MMSET-IN-1 has a Kd of 1.6 μM for MMSET.
  36. RTC-30 is an optimized phenothiazine with anti-cancer potency. RTC-30 contains a hydroxylated linker (N) that confers increased oral bioavailability.
  37. PANK modulator

    PZ-2891 is an orally bioavailable, brain penetrant pantothenate kinase (PANK) modulator. PZ-2891 act as an orthosteric inhibitor at high concentrations and an allosteric activator at lower sub-saturating concentrations. PZ-2891 inhibits human pantothenate kinases PANK1β, PANK2, and PANK3 with IC50s of 40.2 nM, 0.7 nM and 1.3 nM, respectively.
  38. MYOF inhibitor

    WJ460 is an inhibitor of myoferlin (MYOF) which exerts anti-metastatic activity in the nanomolar range in breast cancer cells.
  39. Tyclopyrazoflor is an anthranilamide compound with pesticidal activity.
  40. SBI-477 is a chemical probe stimulated insulin signaling by deactivating the transcription factor MondoA, leading to reduced expression of the insulin pathway suppressors thioredoxin-interacting protein (TXNIP) and arrestin domain?Ccontaining 4 (ARRDC4).
  41. nucleoside transport inhibitor

    Soluflazine is a nucleoside transport inhibitor with anticonvulsant action. Soluflazine can be used as an antiepileptic agent.
  42. DMT1 inhibitor

    DMT1 blocker 2, Compound 12f, is a direct inhibitor of divalent metal transporter 1 (DMT1) with an IC50 of 0.83 μM, is expected to block iron uptake by enterocytes in vivo.
  43. DMT1 blocker

    DMT1 blocker 1 is a blocker of divalent metal transporter 1 (DMT1) with an IC50 of 0.64 μM, is expected to block iron uptake by enterocytes in vivo.
  44. Rolziracetam is a nootropic drug of the racetam family and improves short-term memory in rats and monkeys.
  45. DPD inhibitor

    TAS-114 is a dual dUTPase/dihydropyrimidine dehydrogenase (DPD) inhibitor, can improving the therapeutic efficacy of fluoropyrimidine.
  46. Neridronate is an aminobisphosphonate, licensed in Italy for the treatment of osteogenesis imperfecta (OI) and Paget??s disease of bone (PDB). Neridronate is effective also in other skeletal diseases such as osteoporosis, algodystrophy, hypercalcemia of malignancy, and bone metastases.
  47. Tridentate Fe-chelating agent

    Pyridoxal isonicotinoyl hydrazone (PIH) is a lipophilic, tridentate Fe-chelating agent that shows high Fe chelation efficacy.
  48. p27(Kip1) inhibitor

    SJ572403 (SJ403) is an inhibitor of disordered protein p27(Kip1). p27(Kip1) is a regulator of the CDKs that control eukaryotic cell division.
  49. SEC inhibitor

    SEC inhibitor KL-2 (KL-2), a peptidomimetic lead compound, is a potent, selective super elongation complex (SEC) inhibitor and disrupts the interaction between the SEC scaffolding protein AFF4 and P-TEFb, resulting in impaired release of Pol II from promoter-proximal pause sites and a reduced average rate of processive transcription elongation.
  50. Lipoamidase substrate

    L-Lysine thioctate is a substrate of lipoamidase.

Items 551-600 of 980

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