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CXCR4 Inhibitor
MSX-122 is an orally bioavailable inhibitor of CXCR4 (IC50 = ~10 nM) with potential antineoplastic and antiviral activities. CXCR4 inhibitor MSX-122 binds to the chemokine receptor CXCR4, preventing the binding of stromal derived factor-1 (SDF-1) to the CXCR4 receptor and receptor activation, which may result in decreased tumor cell proliferation and migration. -
LRRK2 kinase inhibitor
GSK2578215A is a potent leucine-rich repeat kinase 2 (LRRK2) inhibitor (IC50 values are 8.9 and 10.1 nM respectively for LRRK2[G2019S] mutant and wild-type LRRK2 respectively). -
LRRK2 Inhibitor III
HG-10-102-01 is a brain penetrant, potent and selective inhibitor of wild-type LRRK2. -
Autophagy Inhibitor
Spautin-1 is a novel autophagy inhibitor, IM inhibited the growth of K562 cells with IC50 of 1.03μM. In contrast, co-treatment with Spautin-1 increased IM-induced inhibition of cell viability with IC50 of 0.45 μM.- Yoon-Jin Kim, .et al. , Sci Adv, 2021, Feb 19;7(8) PMID: 33608268
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CXCR4 antagonist
Plerixafor is an immunostimulant used to multiply hematopoietic stem cells and it is a chemokine receptor-4 antagonist for mobilization of hematopoietic stem cells for transplantation.- Hitoshi Maeda, .et al. , Int J Biol Macromol, 2022, Sep 17;221:1439-1452 PMID: 36126807
- Jingying Chen, .et al. , Development, 2022, Jul 1;149(13) PMID: 35694896
- Narubhorn Ongprakobkul, .et al. , Am J Orthod Dentofacial Orthop, 2022, Mar 2;S0889-5406(22)00107-X PMID: 35248418
- Chunliang Liu, .et al. , J Trace Elem Med Biol, 2022, Jan 10;71:126927 PMID: 35030482
- Eri Watanabe, .et al. , Angiogenesis, 2020, Jul 22 PMID: 32699964
- Alessandra Esposito, .et al. , Bone, 2020, Jul 3;139:115521 PMID: 32629173
- Kentaro Suzuki, .et al. , Sci Rep, 2019, 9: 15284
- Ichimizu S, .et al. , J Control Release, 2019, May 10;304:156-163 PMID: 31082432
- Nan Li, .et al. , Diagn Pathol, 2019, Jan 12;14(1):3 PMID: 30636642
- Thida W, .et al. , Biochem Biophys Res Commun, 2018, Nov 20. pii: S0006-291X(18)32477-X PMID: 30470571
- Henry R. Hampton, .et al. , Nat Commun, 2015, 6: 7139 PMID: 25972253
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LRRK2 inhibitor
CZC-25146 is a potent and selective LRRK2 inhibitor. CZC-25146 prevents mutant LRRK2-induced injury of cultured rodent and human neurons with mid-nanomolar potency. -
LRRK2 inhibitor
GNE-9605 is a highly potent and selective leucine-rich repeat kinase 2 (LRRK2) inhibitor with Ki and IC50 of 2 nM and 19 nM, respectively.- Vijaya Bharti, .et al. , Cell Rep, 2022, Dec 20;41(12):111826 PMID: 36543138
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CXCR2 antagonist
SB 265610 is a nonpeptide, allosteric, inverse agonist of CXCR2 (Kd = 2.51 nM) that prevents receptor activation by binding to a region distinct from the agonist binding site. It does not bind to the related CXCR1 receptor.1 It has been shown to prevent neutrophil chemotaxis both in vitro and in a rat model of hyperoxia-induced lung injury. - Hydroxychloroquine Sulfate is an antimalarial agent used for the treatment of systemic lupus erythematosus, rheumatoid arthritis and other autoimmune, inflammatory and dermatologic conditions. Also acts as an inhibitor of autophagy and toll-like receptor (TLR) 7/9.
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DRP1 inhibitor
Mdivi-1 is a selective cell-permeable inhibitor of mitochondrial division DRP1 (dynamin-related GTPase) and mitochondrial division Dynamin I (Dnm1) with IC50 of 1-10 uM.- Umut Kerem Kolac, .et al. , Mol Biol Rep, 2023, Jan;50(1):493-506 PMID: 36352179
- KOLAC UK, .et al. , Research Square, 2022, 03 Jun
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Glutaminase inhibitor
CB-839 an is orally bioavailable inhibitor of glutaminase, with potential antineoplastic activity. CB-839 (Telaglenastat) also inudces autophagy and has antitumor activity.
- Beatriz Giesen, .et al. , Pharmaceutics, 2021, Feb 23;13(2):295 PMID: 33672398
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Topoisomerase II inhibitor
Doxorubicin is an antibiotic agent that inhibits DNA topoisomerase II and induces DNA damage and apoptosis.- Laura Wiggins, .et al. , Nat Commun, 2023, 14: 1854
- Stefania Scialla, .et al. , Int J Pharm, 2023, Feb 5;632:122575 PMID: 36603672
- Fernando Espinola-Portilla, .et al. , Mol. Pharmaceutics, 2023, 20(3): 1490-1499
- Vijaya Bharti, .et al. , Cell Rep, 2022, Dec 20;41(12):111826 PMID: 36543138
- R Mahalakshmi, .et al. , Mol Biol Rep, 2022, Jan;49(1):463-476 PMID: 34739690
- J Priyanga, .et al. , Chem Biol Interact, 2020, Nov 1;331:109250 PMID: 32956706
- Abdelrehim A, .et al. , PLoS One, 2019, Feb 22;14(2):e0212701 PMID: 30794671
- J Wei, .et al. , bioRxiv, 2018, 2018
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JAK inhibitor
S-Ruxolitinib is the chirality of INCB018424, is a potent and selective small-molecule Janus kinase 1 (JAK1) and JAK2 inhibitor. -
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. -
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. -
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. -
ULK1 inhibitor
SBI-0206965 is a potent, selective and cell permeable autophagy kinase ULK1 inhibitor with IC50 of 108 nM for ULK1 kinase activity and 711 nM for the highly related kinase ULK2 .- SR Bonam, .et al. , Cells, 2020, May; 9(5): 1321 PMID: 32466347
- Altea Rocchi, .et al. , PLoS Genet, 2017, Aug; 13(8): e1006962 PMID: 28806762
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Autophagy inhibitor
Lys05 is a potent lysosomal autophagy inhibitor. Lys05 is a previously undescribed dimeric chloroquine which more potently accumulates in the lysosome and blocks autophagy compared with HCQ. - Azithromycin Dihydrate is an acid stable orally administered macrolide antimicrobial drug, structurally related to erythromycin.
- Chloroquine phosphate is a 4-aminoquinoline anti-malarial and anti-rheumatoid agent, also acting as an ATM activator.
- Vijaya Bharti, .et al. , Cell Rep, 2022, Dec 20;41(12):111826 PMID: 36543138
- Egawa Y, .et al. , PLoS One, 2018, Jun 7;13(6):e0198940 PMID: 29879220
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glucocorticoid receptor agonist
Dexamethasone acetate (Dexamethasone 21-acetate) is a glucocorticoid receptor agonist. -
GPR35/CXCR8 agonist
Kynurenic acid, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid is also an agonist of GPR35/CXCR8. - Sevelamer hydrochloride is a phosphate binding drug used to treat hyperphosphatemia in patients with chronic kidney disease; consists of polyallylamine that is crosslinked with epichlorohydrin.
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glucocorticoid receptor agonist
Dexamethasone Phosphate disodium is a is a water-soluble form of the synthetic glucocorticoid dexamethasone. -
Autophagy inhibitor
Autophinib is a novel potent autophagy inhibitor, inhibiting autophagy induced by starvation or Rapamycin by targeting the lipid kinase VPS34. -
tricyclic antidepressant
Nortriptyline hydrochloride (Desmethylamitriptyline hydrochloride) is a tricyclic antidepressant and the main active metabolite of Amitriptyline, and used to relieve the symptoms of depression. - Lumefantrine, also known as HSDB 7210, is an antimalarial agent used to treat acute uncomplicated malaria. It is administered in combination with artemether for improved efficacy. This combination therapy exerts its effects against the erythrocytic stages of Plasmodium spp. and may be used to treat infections caused by P. falciparum and unidentified Plasmodium species, including infections acquired in chloroquine-resistant areas.
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HDAC inhibitor
Valproic acid is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2; Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches.- Dan Zhao, .et al. , Poult Sci, 2022, Mar; 101(3): 101642 PMID: 35016046
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nucleoside analog
Cytarabine hydrochloride, a nucleoside analog, causes S phase cell cycle arrest and inhibits DNA polymerase. Cytarabine inhibits DNA synthesis with an IC50 of 16 nM. -
CoA reductase inhibitor
Atorvastatin, (+/-)- is a Hydroxymethylglutaryl-CoA reductase inhibitor. -
iron chelator
Deferoxamine mesylate is an iron chelator that binds free iron in a stable complex, preventing it from engaging in chemical reactions. -
multi-targeted receptor tyrosine kinase inhibitor
Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively.- Wei Kang Cheng, .et al. , Microvasc Res, 2022, Feb 11;142:104341 PMID: 35157839
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glucocorticoid receptor agonist
Dexamethasone palmitate (DXP) is a prodrug of Dexamethasone, which is a glucocorticoid receptor agonist. Dexamethasone palmitate (DXP) has a 47-fold lower affinity for the glucocorticoid receptor than Dexamethasone. Anti-inflammatory agent. -
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.