Autophagy Signaling

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  1. CaM-KK inhibitor

    STO-609 is a selective and cell-permeable inhibitor of the Ca2+/calmodulin-dependent protein kinase kinase (CaM-KK), with Ki values of 80 and 15 ng/mL for recombinant CaM-KKα and CaM-KKβ, respectively.
  2. Heme oxygenase (HO)-1 inducer

    Hemin is an iron-containing porphyrin. Hemin is an Heme oxygenase (HO)-1 inducer.
  3. CXCR2 antagonist

    Danirixin is a selective, and reversible CXCR2 antagonist, with IC50?of?12.5 nM for CXCL8.
  4. rapamycin enhancer/autophagy inducer

    SMER18 is a small molecule enhancer of rapamycin which act as a mTOR-independent autophagy inducer.
  5. Arglabin is a sesquiterpene gamma-lactone is isolated from Artemisia glabella; anticancer natural compound.
  6. Heparin is a highly sulfated glycosaminoglycan,that is widely used as an injectable anticoagulant, and has the highest negative charge density of any known biological molecule.
  7. CYP26 inhibitor/RAMBA

    Talarozole (R115866) is an oral systemic all-trans retinoic acid metabolism blocking agent (RAMBA) which increases intracellular levels of endogenous all-trans retinoic acid (RA). Talarozole inhibits both CYP26A1 and CYP26B1 with IC50s of 5.4 and 0.46 nM, respectively.
  8. CXCR3 antagonist

    NBI-74330 is a potent antagonist for CXCR3, and exhibits potent inhibition of (125I)CXCL10 and (125I)CXCL11 specific binding with Ki of 1.5 and 3.2 nM, respectively.
  9. CXCR3 antagonist

    AMG 487 is an orally active and selective antagonist of CXC chemokine receptor 3 (CXCR3) which inhibits the binding of CXCL10 and CXCL11 to CXCR3 with IC50s of 8.0 and 8.2 nM, respectively.
  10. human CX3CR1 receptor modulator

    AZD8797 is an allosteric non-competitive and orally active modulator of the human CX3CR1 receptor; antagonizes CX3CR1 and CXCR2 with Kis of 3.9 and 2800 nM, respectively.
  11. Amiodarone is an antiarrhythmic drug for inhibition of ATP-sensitive potassium channel with an IC50 of 19.1 μM.

  12. AMP-activated protein kinase activator

    AICAR phosphate is an activator of AMP-activated protein kinase (AMPK).
  13. retinoic acid metabolism inhibitor

    (+)-Talarozole is a potent inhibitor of retinoic acid metabolism extracted from patent WO 1997049704 A1.
  14. ULK1 activator

    LYN-1604 hydrochloride is a potent ULK1 activator with an EC50 of 18.94 nM.
  15. retinoic acid metabolism inhibitor

    (-)-Talarozole is a potent inhibitor of retinoic acid metabolism extracted from patent WO 1997049704 A1.
  16. sulfasalazine analog

    Ipsalazide is a novel sulfasalazine analog designed to release 5-aminosalicylic acid and a nontoxic carrier molecule in the gastrointestinal tract.
  17. macroautophagy/autophagy inhibitor

    CA-5f is a potent late-stage macroautophagy/autophagy inhibitor via inhibiting autophagosome-lysosome fusion.
  18. Oxyphenisatin acetate, the pro-drug of oxyphenisatin, is used to be a laxative.
  19. LRRK2 inhibitor

    LRRK2 inhibitor 1 is a potent, selective and oral LRRK2 inhibitor with an pIC50 of 6.8 nM.
  20. Guggulsterone is a plant sterol derived from the gum resin of the tree Commiphora wightii. Guggulsterone inhibits the growth of a wide variety of tumor cells and induces apoptosis through down regulation of antiapoptotic gene products (IAP1, xIAP, Bfl-1/A1, Bcl-2, cFLIP and survivin), modulation of cell cycle proteins (cyclin D1 and c-Myc), activation of caspases and JNK, inhibition of Akt.
  21. GPR35/CXCR8 antagonist

    ML 145 is a selective GPR35/CXCR8 antagonist with an IC50/EC50 of 20.1 nM, but not for the related GPR55 orphan receptor. GPR35 is expressed by various cells of the immune system and it may has potential as a therapeutic target in inflammatory disease.
  22. GPR35/CXCR8 agonist

    Kynurenic acid sodium, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid sodium is also an agonist of GPR35/CXCR8.
  23. Lysosomotropic autophagy inhibitor

    IITZ-01 is a potent lysosomotropic autophagy inhibitor with single-agent antitumor activity, with an IC50 of 2.62 μM for PI3Kγ.
  24. Nrf2 activator

    TBHQ (tert-Butylhydroquinone) is a widely used Nrf2 activator, protects against Doxorubicin (DOX)-induced cardiotoxicity through activation of Nrf2.
  25. CXCR4 antagonist

    IT1t is a potent CXCR4 antagonist; inhibits CXCL12/CXCR4 interaction with an IC50 of 2.1 nM.
  26. Urolithin A, a gut-microbial metabolite of ellagic acid, exerts anti-inflammatory, antiproliferative, and antioxidant properties. Urolithin A induces autophagy and apoptosis, suppresses cell cycle progression, and inhibits DNA synthesis.
  27. EN6

    Autophagy activator

    EN6 is a novel covalent autophagy activator, targeting cysteine 277 in the ATP6V1A subunit of the lysosomal v-ATPase, which activates mTORC1 via the Rag guanosine triphosphatases.
  28. Xanthocillin is a marine agent extracted from Penicillium commune, induces autophagy through inhibition of the MEK/ERK pathway.
  29. autophagy receptor

    ALLO-1, an autophagy receptor, is essential for autophagosome formation around paternal organelles and directly binds to the worm LC3 homologue LGG-1 through its LC3-interacting region (LIR) motif.
  30. CXCR4 receptor antagonist

    USL311 is a CXCR4 receptor antagonist which prevents the binding of stromal-cell derived factor-1 (SDF-1 or CXCL12) to CXCR4.
  31. LRRK2 inhibitor

    PFE-360, also known asd PF-06685360, is a potent and selective inhibitor of LRRK2 kinase.
  32. Autophagy inhibitor

    Aumitin is an autophagy inhibitor, targeting mitochondrial complex I. Aumitin inhibits starvation- and rapamycin induced autophagy dose dependently with IC50s of 0.12 μM and 0.24 μM, respectively.
  33. mitophagy regulator

    P62-mediated mitophagy inducer is a mitophagy regulator which activates mitophagy without recruiting Parkin or collapsing δ??m and retains activity in cells devoid of a fully functional PINK1/Parkin pathway.
  34. Autophagy inhibitor

    EACC is a reversible autophagy inhibitor, which can block autophagic flux. EACC selectively inhibits the translocation of autophagosome-specific SNARE Stx17 thereby blocking autophagosome-lysosome fusion.
  35. drug-linker conjugate for ADC

    AmPEG6C2-Aur0131 is a drug-linker conjugate for ADC (anti-CXCR4 ADC) with potent antitumor activity by using Aur0131 (an auristatin microtubule inhibitor), linked via the non-cleavable linker AmPEG6C2.
  36. drug-linker conjugate for ADC

    AcLys-PABC-VC-Aur0101 is a drug-linker conjugate for ADC (anti-CXCR4 ADC) with potent antitumor activity by using Aur0101 (an auristatin microtubule inhibitor), linked via the cleavable linker AcLys-PABC-VC.
  37. Human CXCR3 agonist

    PS372424, a three amino-acid fragment of CXCL10, is a specific human CXCR3 agonist with anti-inflammatory activity, which inhibits the binding of CXCR3 ligand CXCL10 to CXCR3 receptor with IC50 of 42 nM.
  38. CXCR7 modulator

    CXCR7 modulator 1 (compound 25) is a potent and orally bioavailable peptoid hybrid CXCR7 modulator, with a Ki of 9 nM.
  39. Cholesterol biosynthesis inhibitor

    Monacolin J is an inhibitor of cholesterol biosynthesis, and inhibits the activity of HMG-CoA reductase.
  40. Polydatin, a natural precursor of resveratrol, induces β-defensin production and reduces inflammatory response.
  41. JAK inhibitor

    S-Ruxolitinib is the chirality of INCB018424, is a potent and selective small-molecule Janus kinase 1 (JAK1) and JAK2 inhibitor.
  42. CXCR4 antagonist

    AMD-070 hydrochloride is a potent and selective antagonist of CXCR4 with an IC50 value of 13 nM in a CXCR4 125I-SDF inhibition binding assay, inhibit the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs.
  43. CXCL8 receptor inhibitor

    Reparixin L-lysine salt is an inhibitor of CXCL8 receptor, also inhibit CXCR1 and CXCR2 activation,which has been shown to attenuate inflammatory responses in various injury models.
  44. CXCL chemokines antagonist

    UNBS5162 is a novel naphthalimide that decreases CXCL chemokine expression in experimental prostate cancers; the mean antiproliferative activity IC50 value is 17.9 uM for 9 cancer cell lines; hydrolysis product of UNBS3157.
  45. EGFR inhibitor

    AV-412 (MP412) is an EGFR inhibitor with IC50s of 0.75, 0.5, 0.79, 2.3, 19 nM for EGFR, EGFRL858R, EGFRT790M, EGFRL858R/T790M and ErbB2, respectively.
  46. LRRK2 inhibitor

    PF-06447475 is a highly potent, selective, brain penetrant LRRK2 inhibitor with IC50 of 3 nM/11 nM for Wt LRRK2/G2019S LRRK2 respectively.
  47. LRRK2 inhibitor

    CZC-54252 is a potent inhibitor of LRRK2 with IC50s of 1.28 nM and 1.85 nM for wild-type and G2019S LRRK2 respectively.
  48. anti-cancer agent

    Falcarindiol (FAD, (3R,8S)-Falcarindiol, FaDOH) is a natural polyacetylene compound found rich in many plants of the Umbelliferae family. Falcarindiol suppresses LPS-stimulated expression of inducible nitric oxide synthase (iNOS), tumor necrosis factor alpha (TNFα), interleukin-6 (IL-6), and interleukin-1 beta (IL-1β). Falcarindiol attenuates the LPS-induced activation of JNK, ERK, STAT1, and STAT3 signaling molecules. Falnidamol is a pyrimido-pyrimidine compound with anti-cancer activity.
  49. anti-bacterial agent

    Pogostone is isolated from patchouli with anti-bacterial and anti-cancer activities. Pogostone inhibits both gram negative and gram positive bacteria, also show inhibitory effect on corynebacterium xerosis with a MIC value of 0.098 ?g/ml . Pogostone induces cell apoptosis and autophagy.

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