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EPZ015666 - 98% (HPLC), high purity , CAS No.1616391-65-1, Inhibitor of protein arginine methyltransferase 5

  • ≥98%(HPLC)
Item Number
E167694
Grouped product items
SKUSizeAvailabilityPrice Qty
E167694-5mg
5mg
In stock
$107.90
E167694-25mg
25mg
In stock
$486.90
E167694-50mg
50mg
In stock
$489.90
E167694-100mg
100mg
In stock
$706.90

Selective, potent PRMT5 inhibitor

Basic Description

Synonyms(S)-N-(3-(3,4-Dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)-6-(oxetan-3-ylamino)pyrimidine-4-carboxamide,GSK3235025,YQ36286
Specifications & Purity98% (HPLC)
Storage TempStore at -20°C
Shipped InDry ice
Action TypeINHIBITOR
Mechanism of actionInhibitor of protein arginine methyltransferase 5

Associated Targets

PRMT5 Tchem Protein arginine N-methyltransferase 5 3 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

IUPAC Name N-[(2S)-3-(3,4-dihydro-1H-isoquinolin-2-yl)-2-hydroxypropyl]-6-(oxetan-3-ylamino)pyrimidine-4-carboxamide
INCHI InChI=1S/C20H25N5O3/c26-17(10-25-6-5-14-3-1-2-4-15(14)9-25)8-21-20(27)18-7-19(23-13-22-18)24-16-11-28-12-16/h1-4,7,13,16-17,26H,5-6,8-12H2,(H,21,27)(H,22,23,24)/t17-/m0/s1
InChi Key ZKXZLIFRWWKZRY-KRWDZBQOSA-N
Canonical SMILES C1CN(CC2=CC=CC=C21)CC(CNC(=O)C3=CC(=NC=N3)NC4COC4)O
Isomeric SMILES C1CN(CC2=CC=CC=C21)C[C@H](CNC(=O)C3=CC(=NC=N3)NC4COC4)O
PubChem CID 90241673
Molecular Weight 383.44

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Certificate of Analysis(COA)

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4 results found

Lot NumberCertificate TypeDateItem
J2226404Certificate of AnalysisAug 22, 2022 E167694
J2226410Certificate of AnalysisAug 22, 2022 E167694
J2226419Certificate of AnalysisAug 22, 2022 E167694
J2226526Certificate of AnalysisAug 22, 2022 E167694

Related Documents

References

1. Branscombe TL, Frankel A, Lee JH, Cook JR, Yang Z, Pestka S, Clarke S.  (2001)  PRMT5 (Janus kinase-binding protein 1) catalyzes the formation of symmetric dimethylarginine residues in proteins..  J Biol Chem,  276  (35): (32971-6).  [PMID:11413150]
2. Pal S, Baiocchi RA, Byrd JC, Grever MR, Jacob ST, Sif S.  (2007)  Low levels of miR-92b/96 induce PRMT5 translation and H3R8/H4R3 methylation in mantle cell lymphoma..  EMBO J,  26  (15): (3558-69).  [PMID:17627275]
3. Copeland RA.  (2013)  Molecular pathways: protein methyltransferases in cancer..  Clin Cancer Res,  19  (23): (6344-50).  [PMID:23958745]
4. Chung J, Karkhanis V, Tae S, Yan F, Smith P, Ayers LW, Agostinelli C, Pileri S, Denis GV, Baiocchi RA et al..  (2013)  Protein arginine methyltransferase 5 (PRMT5) inhibition induces lymphoma cell death through reactivation of the retinoblastoma tumor suppressor pathway and polycomb repressor complex 2 (PRC2) silencing..  J Biol Chem,  288  (49): (35534-47).  [PMID:24189068]
5. Park JH, Szemes M, Vieira GC, Melegh Z, Malik S, Heesom KJ, Von Wallwitz-Freitas L, Greenhough A, Brown KW, Zheng YG et al..  (2015)  Protein arginine methyltransferase 5 is a key regulator of the MYCN oncoprotein in neuroblastoma cells..  Mol Oncol,  (3): (617-27).  [PMID:25475372]
6. Li Y, Chitnis N, Nakagawa H, Kita Y, Natsugoe S, Yang Y, Li Z, Wasik M, Klein-Szanto AJ, Rustgi AK et al..  (2015)  PRMT5 Is Required for Lymphomagenesis Triggered by Multiple Oncogenic Drivers..  Cancer Discov,  (3): (288-303).  [PMID:25582697]
7. Stopa N, Krebs JE, Shechter D.  (2015)  The PRMT5 arginine methyltransferase: many roles in development, cancer and beyond..  Cell Mol Life Sci,  72  (11): (2041-59).  [PMID:25662273]
8. Yang F, Wang J, Ren HY, Jin J, Wang AL, Sun LL, Diao KX, Wang EH, Mi XY.  (2015)  Proliferative role of TRAF4 in breast cancer by upregulating PRMT5 nuclear expression..  Tumour Biol,  36  (8): (5901-11).  [PMID:25704480]
9. Alinari L, Mahasenan KV, Yan F, Karkhanis V, Chung JH, Smith EM, Quinion C, Smith PL, Kim L, Patton JT et al..  (2015)  Selective inhibition of protein arginine methyltransferase 5 blocks initiation and maintenance of B-cell transformation..  Blood,  125  (16): (2530-43).  [PMID:25742700]

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