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TRK, ROS1, ALK inhibitor
Entrectinib, also known as RXDX-101 and NMS-E628, is an oral small molecule inhibitor of TrkA, TrkB and TrkC, as well as ROS1 and ALK, with high potency and selectivity.- Angelina T Regua, .et al. , Cancer Lett, 2024, Jun 7:597:217023 PMID: 38852701
- Hydrocortisone is a steroid hormone or glucocorticoid produced by the adrenal gland.
- Anumitha Venkatraman, .et al. , J Voice, 2025, 12:S0892-1997(25)00239-5 PMID: 40653410
- Xijian Wang, .et al. , 3 Biotech, 2020, Sep;10(9):377 PMID: 32802719
- Huo, G, .et al. , Appl. Phys. A, 2020, 126, 111
- Zhang J, .et al. , 3 Biotech, 2020, Feb;10(2):35 PMID: 31988829
- Xiucui Bao, .et al. , J Anal Methods Chem, 2019, Article ID 5676159
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HPGDS inhibitor
HPGDS inhibitor 1 is a novel and selective Hematopoietic Prostaglandin D Synthase (HPGDS) inhibitor with an IC50 Value of 0.7 nM.- Beixian Zhou, .et al. , Chin Med, 2023, Oct 27;18(1):139 PMID: 37891648
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HO-1 inhibitor
Zinc Protoporphyrin (Zn(II)-protoporphyrin IX) is a competitive heme oxygenase-1 (HO-1) inhibitor, markedly attenuates the protective effects of Phloroglucinol (PG) against H2O2.- Beixian Zhou, .et al. , MedComm, 2024, Apr 12;5(4):e531 PMID: 38617435
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NOX1/4 inhibitor
GKT137831 is a first in class inhibitor targeting NOX1 and NOX4 enzymes.- Chia-Hui Huang, .et al. , Toxicol Appl Pharmacol, 2020, Apr 17;397:115013 PMID: 32305283
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TLR7 agonist
Imiquimod (Aldara) is a a heterocyclic imidazoquinoline amide that acts as an immune response modifier.- David Diaz-Carballo, .et al. , Commun Biol, 2021, Mar 3;4(1):276 PMID: 33658617
- Kunishita Y, .et al. , Front Immunol, 2020, Feb 7;11:98 PMID: 32117252
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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.- Federico Antoniciello, .et al. , Front Mol Biosci, 2023, May 11;9:887564 PMID: 35647033
- Mei Zheng, .et al. , Biomed Pharmacother, 2022, Jun;150:112996 PMID: 35462338
- Asiedu KO, .et al. , EJNMMI Res, 2018, Dec 13;8(1):109 PMID: 30547233
- Kingsley O. Asiedu, .et al. , Clin Cancer Res, 2017, Jun 1; 23(11): 2759-2768 PMID: 27965305
- Mifamurtide is a liposomal formulation containing a muramyl dipeptide (MDP) analogue with potential immunomodulatory and antineoplastic activities
- François A. Simard, .et al. , Oncoimmunology, 2017, 6(2): e1265716 PMID: 28344871
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COX-1 inhibitor
(-)-Epicatechin is a natural product from green tea. (-)Epicatechin is an inhibitor of Cox-1- Grace Northrop, .et al. , Food Funct, 2022, Apr 4;13(7):3894-3904 PMID: 35285840
- A S D'Costa, .et al. , Food Chem, 2020, Oct 1;341(Pt 2):128256 PMID: 33035827
- Mihaela Tudorache, .et al. , Food Hydrocoll, 2019, 97, Dec, 105193
- Md Shajedul Islam, .et al. , Innovative food science & emerging technologies, 2016, v.34 pp. 344-351
- Islam MS, .et al. , J Agric Food Chem, 2016, Oct 10 PMID: 27632812
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Hsp90/SRC/COX-2 Inhibitor
Radicicol is a potent inhibitor of Hsp90, SRC, and Cox-2- Guangsen Li, .et al. , Pharm Biol, 2023, 61(1): 271-280 PMID: 36655371
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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.- Helen C Wang, .et al. , Cell Rep, 2024, Aug 27;43(8):114542 PMID: 39046877
- 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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TLR7/8 Agonist
Resiquimod is an immune response modifier that acts as a potent TLR 7/8 agonist. Phase 2.- Honglin Huang, .et al. , Acta Pharmaceutica Sinica B, 2023, Ocb,26
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Acetylcysteine is a pharmaceutical drug and nutritional supplement used primarily as a mucolytic agent and in the management of paracetamol (acetaminophen) overdose. Oral acetylcysteine is also used for the prevention of radiocontrast-induced nephropathy (a form of acute renal failure).
- Hua Xu, .et al. , Cancers (Basel), 2020, Apr; 12(4): 831 PMID: 32235588
- R Kasi, .et al. , Clinical Cancer Drugs, 2020, 2019, 7(1): 44 - 56
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Keap1/Nrf2/ARE pathway inducer
(R)-Sulforaphane is a highly potent inducer of the Keap1/Nrf2/ARE pathway. (R)-Sulforaphane is a far more potent inducer of the carcinogen-detoxifying enzyme systems in rat liver and lung than the S-isomer.- Isin Cakir, .et al. , Elife, 2022, Mar 24 PMID: 35323110
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NFAT inhibitor
NFAT Inhibitor, selective inhibitor of calcineurin-mediated dephosphorylation of nuclear factor of activated T cells (NFAT).- Jingwen Liu, .et al. , Cell Mol Gastroenterol Hepatol, 2021, Jul 1;S2352-345X(21)00135-1 PMID: 34217895
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COX-1 inhibitor
Ibuprofen is a nonsteroidal anti-inflammatory drug (NSAID) targeting COX-1 with an IC50 of 13 μM.- Jingyeong Shin, .et al. , Chemical Engineering Journal, 2023, December
- Azuma T, .et al. , Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. , Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
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Gal-3 inhibitor
GB1107 is a potent, selective, orally active inhibitor of Galectin-3 (Gal-3) with a Kd of 37 nM for human Galectin-3. GB1107 reduces human and mouse lung adenocarcinoma growth and blocks metastasis in the syngeneic model.- Jiten R Sharma, .et al. , Life Sci, 2023, Apr 1;318:121480 PMID: 36775116
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RUNX2-DNA binding inhibitor
CADD522 is a potent inhibitor of runt-related transcription factor-2 (RUNX2)-DNA binding with an IC50 of 10 nM. CADD522 exhibits antitumor activity.- Jiten R Sharma, .et al. , Life Sci, 2023, Apr 1;318:121480 PMID: 36775116
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CXCR4 antagonist
AMD 3465 is a potent, selective CXCR4 antagonist.- Kentaro Suzuki, .et al. , Sci Rep, 2019, 9: 15284
- 6-Thioguanine (Thioguanine; 2-Amino-6-purinethiol) is an anti-leukemia and immunosuppressant agent,
- Kevin Bohm, .et al. , Arch Pharm (Weinheim), 2023, Jul;356(7):e2200661 PMID: 37196427
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COX inhibitor
Acetaminophen (paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 25.8 μM; is a widely used antipyretic and analgesic drug. Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor.- L Wang, .et al. , Physiol Res, 2024, Nov 15;73(5):769-778 PMID: 39545791
- Jingyeong Shin, .et al. , Chemical Engineering Journal, 2023, December
- Takashi Azuma, .et al. , SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Azuma T, .et al. , Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. , Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
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NADPH-oxidase inhibitor
Apocynin is a NADPH oxidase inhibitor- Liling Su, .et al. , Ecotoxicol Environ Saf, 2022, Jun 1;237:113519 PMID: 35453021
- Shimizu S, .et al. , Br J Pharmacol, 2018, Sep;175(18):3727-3737 PMID: 29981238
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NRF2 inhibitor
ML-385 is an inhibitor of nuclear factor erythroid 2-related factor 2 (Nrf2) with IC50 value of 1.9 μM.- Liping Luo, .et al. , Heliyon, 2023, Aug 3;9(8):e18929 PMID: 37600361
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FLAP inhibitor
MK-0591 is a selective and specific 5-Lipoxygenase-activating protein (FLAP) inhibitor with an IC50 value of 1.6 nM in a FLAP binding assay.- MA Sartim, .et al. , Biomolecules, 2020, May; 10(5): 794 PMID: 32443924
- Prostaglandin F2α is a naturally occurring prostaglandin used in medicine to induce labor and as an abortifacient.
- Michel R Corboz, .et al. , Prostaglandins Other Lipid Mediat, 2020, Oct 1;152:106486 PMID: 33011365
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CCR2 antagonist
MK-0812 is a potent and selective CCR2 antagonist with low nM affinity for CCR2 on human monocytes and low nM in the chemotaxis assay. It has good PK profiles in preclinical species and demonstrated efficacy in animal models.- Murakami K, .et al. , Vet Immunol Immunopathol, 2016, Dec;182:52-58 PMID: 27863550
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CXCL8/CXCR1/2 Inhibitor
Reparixin is a potent inhibitor of both CXCL8 receptors CXCR1/2, it inhibits weakly CXCR2-mediated cell migration (IC50=100 nM), whereas it strongly blocks CXCR1-mediated chemotaxis (IC50=1 nM).- Naour AL, .et al. , J Mol Cell Biol, 2019, Sep 3 PMID: 31504643
- Wigenstam E, .et al. , Toxicology, 2015, Feb 3;328:40-7 PMID: 25497111
- Mito-TEMPO is a mitochondria-targeted superoxide dismutase mimetic with superoxide and alkyl radical scavenging properties.
- Panpan Tai, .et al. , J Transl Med, 2023, Nov 17;21(1):823 PMID: 37978379
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COX inhibitor
Etodolac (AY-24236) is a non-steroidal anti-inflammatory compound that is a non-selective inhibitor of COX (IC50=53.5 nM).- Paul Mark Medina, .et al. , Transl Oncol, 2021, Jan;14(1):100940 PMID: 33221682
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TLR Inhibitor
TLR2-IN-C29 is an inhibitor of TLR2/1 and TLR2/6 signaling.- Qian-Lu Wang, .et al. , Mol Immunol, 2021, Oct;138:99-109 PMID: 34365196
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NOS inhibitor
Asymmetric dimethylarginine is an endogenous inhibitor of nitric oxide synthase (NOS), and functions as a marker of endothelial dysfunction in a number of pathological states.- Raul Salinas, .et al. , PLoS One, 2023, Mar 2;18(3):e0282155 PMID: 36862634
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COX inhibitor
Indomethacin is a nonselective COX1 and COX2 inhibitor with IC50 of 0.1 μg/mL and 5 μg/mL, respectively. Indomethacin(Indocid, Indocin) is a non-steroidal anti-inflammatory compound commonly used to reduce fever, pain, stiffness, and swelling.- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- Azuma T, .et al. , Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. , Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
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CCR antagonist
Maraviroc is an antiretroviral drug in the CCR5 receptor antagonist class used in the treatment of HIV infection.- Roman V Uzhachenko, .et al. , Cell Rep, 2021, Apr 6;35(1):108944 PMID: 33826903
- Karampoor S, .et al. , Int Immunopharmacol, 2020, Mar;80:106138 PMID: 32007705
- Taisuke Ito, .et al. , JCIA, 2020, 22 January
- Mycophenolic Acid is an immunosuppressant small molecule isolated as a fermentation product from several Penicillium species.
- Romana Vrzonova, .et al. , FEMS Yeast Res, 2021, Jun 29;21(5):foab034 PMID: 34089318
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CXCR1/CXCR2 antagonist
SCH527123 is a potent and selective antagonist of the human CXCR1 and CXCR2 receptors with IC50 of 42 nM and 3 nM, respectively.- Ruijie Zhang, .et al. , Int J Oncol, 2022, May;60(5):50 PMID: 35315502
- Fu S, .et al. , Int J Oncol, 2018, Jul;53(1):349-357 PMID: 29749433
- Fu S, .et al. , Anticancer Res, 2018, Nov;38(11):6271-6279 PMID: 30396947
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HDAC inhibitor
Sulforaphane activates Nrf2 and inhibits high glucose-induced progression of pancreatic cancer via AMPK dependent signaling. Sulforaphane has shown anti-cancer and anti-inflammatory activities.- Satoshi Endo, .et al. , J Biochem, 2021, Mar 17 PMID: 33729485
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mTOR Inhibitors
Rapamycin (Sirolimus) prevents activation of T cells and B-cells by inhibiting their response to interleukin-2 (IL-2).- Saudatu Faruk, .et al. , J Trace Elem Med Biol, 2025, Sep 6:92:127740 PMID: 40945136
- Saudatu Faruk, .et al. , Biol Trace Elem Res, 2025, May 8 PMID: 40338453
- Saudat Faruk, .et al. , Iron, 2025, March
- Yudong Li, .et al. , J Polym Sci, 2024, 62:2215-2230
- Ross van de Weterin, .et al. , Glia, 2024, Jun 20 PMID: 38899723
- Yuanqin Zhang, .et al. , Cancers (Basel), 2023, Dec 2;15(23):5691 PMID: 38067394
- Amnon Wittenstein, .et al. , PLoS Biol, 2023, Nov 9;21(11):e3002355 PMID: 37943958
- Bopei Cui, .et al. , Signal Transduct Target Ther, 2023, Sep 25;8(1):366 PMID: 37743418
- Hideki Kawasaki, .et al. , J Insect Physiol, 2023, Mar;145:104476 PMID: 36623750
- R Mahalakshmi, .et al. , Mol Biol Rep, 2022, Jan;49(1):463-476 PMID: 34739690
- Yusuke Murase, .et al. , Oncol Rep, 2022, Apr;47(4):61 PMID: 35088890
- Zhichao Wu, .et al. , Cells, 2021, Oct 27;10(11):2912 PMID: 34831135
- Matthew A Schaller, .et al. , JCI Insight, 2021, Sep 22;6(18):e148003 PMID: 34357881
- Matthew A. Schaller, .et al. , bioRxiv, 2021, January 21
- Ashley VanCleave, .et al. , Oncotarget, 2020, Jul 7; 11(27): 2597-2610 PMID: 32676162
- Y Huang, .et al. , Experimental and Therapeutic Medicine, 2020, 20(2), 736-747 PMID: 32742319
- Takuya Hirao, .et al. , Cancer Sci, 2018, Jan; 109(1): 121-131 PMID: 29121435
- Ya-Hui Chen, .et al. , J Diabetes Res, 2016, 2016: 1828071 PMID: 28004006
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COX inhibitor
Pravadoline (WIN 48,098) is antiinflammatory and prostaglandin synthesis inhibitor, acting through inhibition of the enzyme cyclooxygenase (COX).- Sharma P, .et al. , Org Lett, 2016, Feb 5;18(3):412-5 PMID: 26745849
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ERRγ agonist
GSK5182 is a highly selective inverse agonist of estrogen-related receptor γ (ERRγ) with an IC50 of 79 nM and does not interact with other nuclear receptors, including ERRα or ERα.- Shike Zhang, .et al. , Journal of Environmental Sciences, 2024, Oct, 8
- Sen He, .et al. , Toxicology, 2021, May 4;457:152805 PMID: 33961950
- Temoporfin(KW 2345) used in photodynamic therapy for the treatment of squamous cell carcinoma of the head and neck. Target: Others Temoporfin used in photodynamic therapy for the treatment of squamous cell carcinoma of the head and neck. Patients can remain photosensitive for several weeks after treatment.
- Shruti Vig, .et al. , Cancer Drug Resist, 2024, Sep 21:7:35 PMID: 39403604
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NOD-like receptors inhibitor
NOD-IN-1 is a potent mixed inhibitor of nucleotide-binding oligomerization domain (NOD)-like receptors, NOD1 and NOD2, with IC50 of 5.74 μM and 6.45 μM, respectively.- Shuqin Lai, .et al. , Int Immunopharmacol, 2025, Feb 6:147:114036 PMID: 39778279
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COX/LOX inhibitor
Licofelone is a dual COX/LOX inhibitor, being considered as a treatment for osteoarthritis. It may reduce the gastrointestinal toxicity associated with other non-steroidal anti-inflammatory drugs, which only inhibit COX (cyclooxygenase). Licofelone is the first drug to inhibit both.- Silke Neumann, .et al. , Front Immunol, 2016, 7: 537 PMID: 27994586
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glucocorticoid receptor agonist
Dexamethasone is a potent synthetic member of the glucocorticoid class of steroid drugs. It acts as an anti-inflammatory and immunosuppressant. Its potency is about 20-30 times that of the naturally occurring hormone hydrocortisone and 4-5 times of prednisone.- Sudam S Mane, .et al. , J Am Soc Mass Spectrom, 2024, Aug 26 PMID: 39186802
- Ken Kobayashi, .et al. , Cell Tissue Res, 2022, Sep;389(3):501-515 PMID: 35748981
- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- Loxoprofen is a non-steroidal anti-inflammatory drug.
- Takashi Azuma, .et al. , SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
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Berberine hydrochloride was novelly found that it has various beneficial effects on the cardiovascular system and significant anti-inflammatory activities. Berberine can effectively reduce intracellular superoxide levels in LPS-stimulated macrophages. Such a restoration of cellular redox by berberine is mediated by its selective inhibition of gp91phox expression and enhancement of SOD activity.
- Takashi Azuma, .et al. , SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Azuma T, .et al. , Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. , Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
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NLRP3 inhibitor
MCC950 sodium is a potent NLRP3 inflammasome inhibitor that inhibits IL-1beta production with IC50 value of 7.5 nm.- Takemasa Takii, .et al. , mSphere, 2025, 10:e00110-25 PMID: 40387341
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COX-1 Inhibitor
Paradol is the active flavor constituent of the seeds of Guinea pepper (Aframomum melegueta); Paradol has been found to have antioxidative and antitumor promoting effects- Taurin Hughes, .et al. , Int J Biol Macromol, 2021, Jul 1;182:2130-2143 PMID: 34087308
- Lihan Zhao, .et al. , Sci Rep, 2020, Nov 5;10(1):19182 PMID: 33154433
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S1P Receptor antagonist
FTY720 is a derivative of ISP-1 (myriocin), a fungal metabolite of the Chinese herb Iscaria sinclarii as well as a structural analog of sphingosine.- Tina Sepasi, .et al. , Int J Pharm, 2023, Apr 5;636:122815 PMID: 36907279
- Tina Sepasi, .et al. , BioImpacts, 2022, 28 May
- Zengzi Zhou, .et al. , Infect Immun, 2020, Oct 19;88(11):e00281-20 PMID: 32868341
- Mayu Idehara, .et al. , Traditional & Kampo Medicine, 2020, 22 July
- Luwa Yuan, .et al. , Sci Rep, 2019, 9:11156 PMID: 31371790
- Sakai Y, .et al. , Int J Biol Macromol, 2018, Nov 22;124:505-514 PMID: 30471397
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CCR5 antagonist
Vicriviroc Malate is a second generation orally active CCR5 antagonist, which is also a potent inhibitor of HIV-1 entry into target cells, with a mean IC50 =0.46 nM and IC50 =1~10 nM to HIV isolates (n=52).- Tomohiro Nabekura, .et al. , Antimicrob Agents Chemother, 2015, Dec; 59(12): 7666-7670 PMID: 26416870

