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Cat #: V3139 CAS #: 2226515-75-7 Purity ≥ 98%
Description: LLY-284 (LLY284) is a negative control and tool compound for LLY-283. It is a diastereomer of LLY-283 but was much less active. LLY-283 (LLY283) is the first-in-class and selective SAM-competitive inhibitor of PRMT5 (protein arginine methyltransferase 5) with antitumor activity. LLY-283 inhibited PRMT5 enzymatic activity in vitro and in cells with IC50 values of 22 ± 3 and 25 ± 1 nM, respectively. LLY-283 also showed antitumor activity in mouse xenografts when dosed orally and can serve as an excellent probe molecule for understanding the biological function of PRMT5 in normal and cancer cells. PRMT5 is ubiquitously expressed in most tissues and its expression has been shown to be elevated in several cancers including breast cancer, gastric cancer, glioblastoma, and lymphoma. PRMTs binds to the lysine or arginine residues of substrate proteins via the substrate binding groove and SAM via the cofactor binding site.
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Molecular Weight (MW) | 342.36 |
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Molecular Formula | C17H18N4O4 |
CAS No. | 2226515-75-7 |
Storage | -20℃ for 3 years in powder form |
-80℃ for 2 years in solvent | |
Solubility In Vitro | DMSO: > 50 mg/mL |
Water: N/A | |
Ethanol: N/A | |
Solubility In Vivo | N/A |
Synonyms | O[C@H]1[C@H](N2C=CC3=C(N)N=CN=C32)O[C@H]([C@@H](O)C4=CC=CC=C4)[C@H]1O |
Solvent volume to be added | Mass (the weight of a compound) | |||
---|---|---|---|---|
Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
1mM | 2.9209 mL | 14.6045 mL | 29.2090 mL | 58.4180 mL |
5mM | 0.5842 mL | 2.9209 mL | 5.8418 mL | 11.6836 mL |
10mM | 0.2921 mL | 1.4605 mL | 2.9209 mL | 5.8418 mL |
20mM | 0.1460 mL | 0.7302 mL | 1.4605 mL | 2.9209 mL |
This equation is commonly abbreviated as: C1 V1 = C2 V2
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.