1. GPCR/G Protein
    Immunology/Inflammation
    GPCR/G Protein
  2. Histamine Receptor
    Sigma Receptor

UNC0642 (Synonyms: UNC-0642; UNC 0642)

Cat. No.: HY-13980 Purity: 99.89%
Data Sheet SDS Handling Instructions

UNC0642 is a potent and selective G9a/GLP inhibitor, inhibits G9a/GLP with an IC50 of less than 2.5 nM.

For research use only. We do not sell to patients.
UNC0642 Chemical Structure

UNC0642 Chemical Structure

CAS No. : 1481677-78-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO $108 In-stock
5 mg $90 In-stock
10 mg $150 In-stock
50 mg $450 In-stock
100 mg $850 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Description

UNC0642 is a potent and selective G9a/GLP inhibitor, inhibits G9a/GLP with an IC50 of less than 2.5 nM.

IC50 & Target

IC50: less than 2.5 nM (G9a, GLP)[1]

In Vitro

UNC0642 displays high in vitro and cellular potency, low cell toxicity, and excellent selectivity. UNC0642 is competitive with the peptide substrate and non-competitive with the cofactor SAM. The Ki of UNC0642 is determined to be 3.7±1 nM. UNC0642 displays high in vitro potency for GLP (IC50< 2.5 nM), similar to G9a. UNC0642 is more than 300-fold selective for G9a and GLP over a broad range of kinases, GPCRs, transporters, and ion channels. UNC0642 exhibits high potency at reducing the H3K9me2 mark, low cell toxicity, and good separation of functional potency and cell toxicity in a number of cell lines. It reduces clonogenicity in PANC-1 cells, a pancreatic carcinoma cell line[1].

In Vivo

A single intraperitoneal (IP) injection (5 mg/kg) of UNC0642results in a plasma Cmax (maximum concentration) of 947 ng/mL and an AUC (area under the curve) of 1265 hr*ng/mL[1].

References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 1.8292 mL 9.1458 mL 18.2916 mL
5 mM 0.3658 mL 1.8292 mL 3.6583 mL
10 mM 0.1829 mL 0.9146 mL 1.8292 mL
Cell Assay
[1]

MDA-MB-231, PC3, and U2OS cells are treated with inhibitors (UNC0642) for 48 h. Cell viability assays are performed by incubating cells with 0.1 mg/mL of resazurin for 3 – 4 h. Resazurin reduction is monitored with 544 nm excitation, measuring fluorescence at 590 nm. In-cell western assay is performed as described previously[1].

Animal Administration
[1]

Mouse: Standard PK studies are performed using male Swiss albino mice. Plasma and brain concentrations are measured at 0.08, 0.25, 0.5, 1, 2, 4, 8, and 24 h following a single IP injection of UNC0642 at 5 mg/kg. The compound concentration at each time point in plasma or brain is the average value from 3 test animals[1].

References
M.Wt

546.7

Formula

C₂₉H₄₄F₂N₆O₂

CAS No.

1481677-78-4

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
UNC0642
Cat. No.:
HY-13980
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