A PRMT5 inhibitor
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Isomer(s)
43141LLY-284
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LLY-283

Item No. 21596

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
7-[(5R)-5-C-phenyl-β-D-ribofuranosyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine
CAS Number
2040291-27-6
Molecular Formula
C17H18N4O4
Formula Weight
342.4
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 60 mg/mlEthanol: 60 mg/ml
λmax
230, 274 nm
SMILES
O[C@H](C1=CC=CC=C1)[C@@]2([H])O[C@@H](N3C=CC4=C3N=CN=C4N)[C@H](O)[C@@H]2O
InChi Code
InChI=1S/C17H18N4O4/c18-15-10-6-7-21(16(10)20-8-19-15)17-13(24)12(23)14(25-17)11(22)9-4-2-1-3-5-9/h1-8,11-14,17,22-24H,(H2,18,19,20)/t11-,12+,13-,14-,17-/m1/s1
InChi Key
WWOOWAHTEXIWBO-QFRSUPTLSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Cayman Chemical
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    Product Description

    LLY-283 is an inhibitor of protein arginine methyltransferase 5 (PRMT5; IC50 = 22 nM).1 It is selective for PRMT5 over a panel of methyltransferases, including PRMT4, -6, and -7 at 1 μM. It reduces symmetric demethylation of SmBB' in MCF-7 cells (IC50 = 25 nM) and inhibits proliferation of various breast, gastric, hematological, lung, skin, and ovarian cancer cell lines (IC50s = 3-30 nM). LLY-283 (20 mg/kg) inhibits tumor growth in an A375 mouse xenograft model. It also disrupts alternative splicing events in, and inhibits proliferation and self-renewal of, patient-derived glioblastoma stem cells and increases survival in an orthotopic patient-derived xenograft (PDX) mouse model.2 See the Structural Genomics Consortium (SGC) website for more information.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Bonday, Z.Q., Cortez, G.S., Grogan, M.J., et al. LLY-283, a potent and selective inhibitor of arginine methyltransferase 5, PRMT5, with antitumor activity. ACS Med. Chem. Lett. 9(7), 612-617 (2018).

    2. Sachamitr, P., Ho, J.C., Ciamponi, F.E., et al. PRMT5 inhibition disrupts splicing and stemness in glioblastoma. Nat. Commun. 12(1), 979 (2021).