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MedKoo Cat#: 532772 | Name: LLY-283
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

LLY-283 is a potent and selective SAM-competitive chemical probe for PRMT5 (protein arginine methyltransferase 5).

Chemical Structure

LLY-283
LLY-283
CAS#2040291-27-6

Theoretical Analysis

MedKoo Cat#: 532772

Name: LLY-283

CAS#: 2040291-27-6

Chemical Formula: C17H18N4O4

Exact Mass: 342.1328

Molecular Weight: 342.36

Elemental Analysis: C, 59.64; H, 5.30; N, 16.37; O, 18.69

Price and Availability

Size Price Availability Quantity
50mg USD 750.00 2 Weeks
100mg USD 1,250.00 2 Weeks
200mg USD 1,950.00 2 Weeks
1g USD 4,850.00 2 Weeks
2g USD 7,450.00 2 Weeks
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Related CAS #
2040291-27-6
Synonym
LLY-283; LLY 283; LLY283; LM-5179; LM 5179; LM5179.
IUPAC/Chemical Name
(2R,3R,4S,5R)-2-(4-aminopyrrolo[2,3-d]pyrimidin-7-yl)-5-[(R)-hydroxy(phenyl)methyl]oxolane-3,4-diol
InChi Key
WWOOWAHTEXIWBO-QFRSUPTLSA-N
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
SMILES Code
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
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
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 Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
LLY-283 is a potent, selective and oral protein arginine methyltransferase 5 (PRMT5) inhibitor, with an IC50 of 22 nM and a Kd of 6 nM for PRMT5:MEP50 complex, and shows antitumor activity.
In vitro activity:
ROS experiments confirmed that LLY-283 could rescue cisplatin-induced oxidative damage to auditory cells. TUNEL experiments confirmed that LLY-283 could protect cisplatin-induced apoptosis of auditory cells. Meanwhile, LLY-283 could inhibit the expression of PRMT5 in auditory cells induced by cisplatin. Reference: J Clin Lab Anal. 2022 Feb;36(2):e24176. https://pubmed.ncbi.nlm.nih.gov/34997776/
In vivo activity:
The aim of this study was to investigate the effect of LLY-283, a selective inhibitor of protein arginine methyltransferase 5 (PRMT5), on a noise-induced hearing loss (NIHL) mouse model and to identify a potential target for a therapeutic intervention against NIHL. LLY-283 pretreatment before noise exposure notably decreased 4-HNE and caspase-3/7 levels in the cochlear HCs. Reference: Ecotoxicol Environ Saf. 2022 Sep 15;243:113992. https://pubmed.ncbi.nlm.nih.gov/35994911/
Solvent mg/mL mM
Solubility
Water 4.3 12.52
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 342.36 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Zhao B, Zhang D, Sun Y, Lei M, Zeng P, Wang Y, Hong Y, Jiao Y, Cai C. Explore the effect of LLY-283 on the ototoxicity of auditory cells caused by cisplatin: A bioinformatic analysis based on RNA-seq. J Clin Lab Anal. 2022 Feb;36(2):e24176. doi: 10.1002/jcla.24176. Epub 2022 Jan 8. PMID: 34997776; PMCID: PMC8842247. 2. Sachamitr P, Ho JC, Ciamponi FE, Ba-Alawi W, Coutinho FJ, Guilhamon P, Kushida MM, Cavalli FMG, Lee L, Rastegar N, Vu V, Sánchez-Osuna M, Coulombe-Huntington J, Kanshin E, Whetstone H, Durand M, Thibault P, Hart K, Mangos M, Veyhl J, Chen W, Tran N, Duong BC, Aman AM, Che X, Lan X, Whitley O, Zaslaver O, Barsyte-Lovejoy D, Richards LM, Restall I, Caudy A, Röst HL, Bonday ZQ, Bernstein M, Das S, Cusimano MD, Spears J, Bader GD, Pugh TJ, Tyers M, Lupien M, Haibe-Kains B, Artee Luchman H, Weiss S, Massirer KB, Prinos P, Arrowsmith CH, Dirks PB. PRMT5 inhibition disrupts splicing and stemness in glioblastoma. Nat Commun. 2021 Feb 12;12(1):979. doi: 10.1038/s41467-021-21204-5. PMID: 33579912; PMCID: PMC7881162. 3. Liu C, Tang D, Zheng Z, Lu X, Li W, Zhao L, He Y, Li H. A PRMT5 inhibitor protects against noise-induced hearing loss by alleviating ROS accumulation. Ecotoxicol Environ Saf. 2022 Sep 15;243:113992. doi: 10.1016/j.ecoenv.2022.113992. Epub 2022 Aug 19. PMID: 35994911. 4. Bonday ZQ, Cortez GS, Grogan MJ, Antonysamy S, Weichert K, Bocchinfuso WP, Li F, Kennedy S, Li B, Mader MM, Arrowsmith CH, Brown PJ, Eram MS, Szewczyk MM, Barsyte-Lovejoy D, Vedadi M, Guccione E, Campbell RM. LLY-283, a Potent and Selective Inhibitor of Arginine Methyltransferase 5, PRMT5, with Antitumor Activity. ACS Med Chem Lett. 2018 Apr 23;9(7):612-617. doi: 10.1021/acsmedchemlett.8b00014. PMID: 30034588; PMCID: PMC6047023.
In vitro protocol:
1. Zhao B, Zhang D, Sun Y, Lei M, Zeng P, Wang Y, Hong Y, Jiao Y, Cai C. Explore the effect of LLY-283 on the ototoxicity of auditory cells caused by cisplatin: A bioinformatic analysis based on RNA-seq. J Clin Lab Anal. 2022 Feb;36(2):e24176. doi: 10.1002/jcla.24176. Epub 2022 Jan 8. PMID: 34997776; PMCID: PMC8842247. 2. Sachamitr P, Ho JC, Ciamponi FE, Ba-Alawi W, Coutinho FJ, Guilhamon P, Kushida MM, Cavalli FMG, Lee L, Rastegar N, Vu V, Sánchez-Osuna M, Coulombe-Huntington J, Kanshin E, Whetstone H, Durand M, Thibault P, Hart K, Mangos M, Veyhl J, Chen W, Tran N, Duong BC, Aman AM, Che X, Lan X, Whitley O, Zaslaver O, Barsyte-Lovejoy D, Richards LM, Restall I, Caudy A, Röst HL, Bonday ZQ, Bernstein M, Das S, Cusimano MD, Spears J, Bader GD, Pugh TJ, Tyers M, Lupien M, Haibe-Kains B, Artee Luchman H, Weiss S, Massirer KB, Prinos P, Arrowsmith CH, Dirks PB. PRMT5 inhibition disrupts splicing and stemness in glioblastoma. Nat Commun. 2021 Feb 12;12(1):979. doi: 10.1038/s41467-021-21204-5. PMID: 33579912; PMCID: PMC7881162.
In vivo protocol:
1. Liu C, Tang D, Zheng Z, Lu X, Li W, Zhao L, He Y, Li H. A PRMT5 inhibitor protects against noise-induced hearing loss by alleviating ROS accumulation. Ecotoxicol Environ Saf. 2022 Sep 15;243:113992. doi: 10.1016/j.ecoenv.2022.113992. Epub 2022 Aug 19. PMID: 35994911. 2. Bonday ZQ, Cortez GS, Grogan MJ, Antonysamy S, Weichert K, Bocchinfuso WP, Li F, Kennedy S, Li B, Mader MM, Arrowsmith CH, Brown PJ, Eram MS, Szewczyk MM, Barsyte-Lovejoy D, Vedadi M, Guccione E, Campbell RM. LLY-283, a Potent and Selective Inhibitor of Arginine Methyltransferase 5, PRMT5, with Antitumor Activity. ACS Med Chem Lett. 2018 Apr 23;9(7):612-617. doi: 10.1021/acsmedchemlett.8b00014. PMID: 30034588; PMCID: PMC6047023.
1. SGC. LLY-283 A Chemical Probe For PRMT5. Accessed on 05/04/2017. Modified on 05/04/2017. thesgc.org, http://www.thesgc.org/chemical-probes/LLY-283