LLY-283 free base · Synonyms: LLY 283 · LLY283

LLY-283 is an effective and selective inhibitor of protein arginine methyltransferase 5.

For research use only. Not for human or veterinary use.

Target Histone Methyltransferase

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

LLY-283 structure

CAS No.: 2040291-27-6

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
100 mg	USD 425.00	BP-01962-100mg	In stock	Get quote
250 mg	USD 808.00	BP-01962-250mg	In stock	Get quote
500 mg	USD 1,295.00	BP-01962-500mg	In stock	Get quote
1 g	USD 2,075.00	BP-01962-1g	In stock	Get quote
5 g	Inquire	BP-01962-5g	Inquire	Inquire

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Description

LLY-283 is an effective and selective inhibitor of protein arginine methyltransferase 5 (PRMT5) (IC50: 22 nM and a Kd: 6 nM for PRMT5:MEP50 complex). It shows antitumor activity.

Biological activity

In Vitro LLY-283 is a potent, oral and selective arginine methyltransferase 5 (PRMT5) inhibitor, with an IC50 of 22 nM in vitro and 25 nM in cells, as well as a Kd of 6 nM for PRMT5:MEP50 complex in vitro; LLY-283 inhibits the proliferation of A375 cell with an IC50 of 46 nM. In Vivo LLY-283 (20 mg/kg; p.o., QD (once a day)) causes a significant inhibition on tumor growth in mice bearing A375 cells after treatment for 28 days.

Identifiers

SMILES: C1=CC=C(C=C1)[C@H]([C@@H]2[C@H]([C@H]([C@@H](O2)N3C=CC4=C(N=CN=C43)N)O)O)O
InChIKey: WWOOWAHTEXIWBO-QFRSUPTLSA-N

Specifications

MW (average): 342.3492
Formula: C₁₇H₁₈N₄O₄
CAS No.: 2040291-27-6
Physical state: Solid
Color: White to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

References

[1]. Zahid Q. Bonday, et al. LLY-283, a Potent and Selective Inhibitor of Arginine Methyltransferase 5, PRMT5, with Antitumor Activity. ACS Med. Chem. Lett., 2018, 9 (7), pp 612-617.

Same target

Search Histone Methyltransferase

Same research area

Search Cancer