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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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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
Synonyms | (S)-N-(3-(3,4-Dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)-6-(oxetan-3-ylamino)pyrimidine-4-carboxamide,GSK3235025,YQ36286 |
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Specifications & Purity | 98% (HPLC) |
Storage Temp | Store at -20°C |
Shipped In | Dry ice |
Action Type | INHIBITOR |
Mechanism of action | Inhibitor of protein arginine methyltransferase 5 |
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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IUPAC Name | N-[(2S)-3-(3,4-dihydro-1H-isoquinolin-2-yl)-2-hydroxypropyl]-6-(oxetan-3-ylamino)pyrimidine-4-carboxamide |
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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 |
PubChem CID | 90241673 |
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CAS Registry No. | 1616391-65-1 |
RCSB PDB Ligand | 3XV |
Enter Lot Number to search for COA:
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Lot Number | Certificate Type | Date | Item |
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J2226404 | Certificate of Analysis | Aug 22, 2022 | E167694 |
J2226410 | Certificate of Analysis | Aug 22, 2022 | E167694 |
J2226419 | Certificate of Analysis | Aug 22, 2022 | E167694 |
J2226526 | Certificate of Analysis | Aug 22, 2022 | E167694 |
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, 9 (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, 5 (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] |