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LLY-507

Item № 16441
CAS № 1793053-37-8
Purity ≥98%
product image
                (CAS 1793053-37-8)
SIZE PRICE QUANTITY SUBTOTAL
CART TOTAL
     1 mg $45.00 0.00
     5 mg $135.00 0.00
     10 mg $248.00 0.00
     25 mg $551.00 0.00

Pricing updated 2019-07-18. Prices are subject to change without notice.

Description

SMYD2 is a lysine N-methyltransferase that methylates both histones and non-histone proteins, including p53 and retinoblastoma-associated protein.1,2 LLY-507 is a cell-active, small molecule inhibitor of SMYD2 (IC50 = 15 nM).3 It has been shown to inhibit p53 lysine370 monomethylation in KYSE-150 esophageal squamous cell carcinoma cells stably expressing SMYD2 with an IC50 value of 0.6 µM.3 LLY-507 is >100-fold selective for SMYD2 over a panel of 27 protein methyltransferases and non-methyltransferase targets.3 See the Structural Genomics Consortium (SGC) website for more information.

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Technical Information
Formal Name
5-cyano-2'-[4-[2-(3-methyl-1H-indol-1-yl)ethyl]-1-piperazinyl]-N-[3-(1-pyrrolidinyl)propyl]-[1,1'-biphenyl]-3-carboxamide
CAS Number
1793053-37-8
Molecular Formula
C36H42N6O
Formula Weight
574.8
Purity
≥98%
Formulation
A crystalline solid
λmax
227 nm
SMILES
N#CC1=CC(C(NCCCN2CCCC2)=O)=CC(C3=CC=CC=C3N4CCN(CCN5C=C(C)C6=C5C=CC=C6)CC4)=C1
InChI Code
InChI=1S/C36H42N6O/c1-28-27-42(34-11-4-2-9-32(28)34)22-19-40-17-20-41(21-18-40)35-12-5-3-10-33(35)30-23-29(26-37)24-31(25-30)36(43)38-13-8-16-39-14-6-7-15-39/h2-5,9-12,23-25,27H,6-8,13-22H2,1H3,(H,38,43)
InChI Key
PNYRDVBFYVDJJI-UHFFFAOYSA-N

Warning - this product is not for human or veterinary use.

Shipping & Storage
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Stability
≥ 2 years
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Additional Information

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References & Product Citations
Product Description References

1. Abu-Farha, M., Lambert, J.P., Al-Madhoun, A.S., et al. The tale of two domains: Proteomics and genomics analysis of SMYD2, a new histone methyltransferase Molecular & Cellular Proteomics 7(3), 560-572 (2008).

2. Brown, M.A., Sims, R.J., III, Gottlieb, P.D., et al. Identification and characterization of Smyd2: A split SET/MYND domain-containing histone H3 lysine 36-specific methyltransferase that interacts with the Sin3 histone deacetylase complex Molecular Cancer 5, 26 (2006).

3. Lee, K., Lee, J.H., Boovanahalli, S.K., et al. (Aryloxyacetylamino)benzoic acid analogues: A new class of hypoxia-inducible factor-1 inhibitors Journal of Medicinal Chemistry 50, 1675-1684 (2007).

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