| Identification | Back Directory | [Name]
UNC-0642 | [CAS]
1481677-78-4 | [Synonyms]
UNC0642
CS-1714
UNC-0642
UNC 0642
UNC-0642;UNC0642;UNC 0642
2-(4,4-difluoropiperidin-1-yl)-N-(1-isopropylpiperidin-4-yl)-6-methoxy-7-(3-(pyrrolidin-1-yl)propoxy)quinazolin-4-amine
2-(4,4-Difluoropiperidin-1-yl)-6-methoxy-N-[1-(propan-2-yl)piperidin-4-yl]-7-[3-(pyrrolidin-1-yl)propoxy]quinazolin-4-amine
2-(4,4-Difluoro-1-piperidinyl)-6-methoxy-N-[1-(1-methylethyl)-4-piperidinyl]-7-[3-(1-pyrrolidinyl)propoxy]-4-quinazolinamine
4-Quinazolinamine, 2-(4,4-difluoro-1-piperidinyl)-6-methoxy-N-[1-(1-methylethyl)-4-piperidinyl]-7-[3-(1-pyrrolidinyl)propoxy]-
UNC0642, 2-(4,4-Difluoro-1-piperidinyl)-6-Methoxy-N-[1-(1-Methylethyl)-4-piperidinyl]-7-[3-(1-pyrrolidinyl)propoxy]-4-quinazolinaMine | [Molecular Formula]
C29H44F2N6O2 | [MDL Number]
MFCD28044322 | [MOL File]
1481677-78-4.mol | [Molecular Weight]
546.7 |
| Chemical Properties | Back Directory | [Boiling point ]
679.2±65.0 °C(Predicted) | [density ]
1.23±0.1 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
Soluble to 100 mM in DMSO and to 50 mM in 1eq. HCl | [form ]
powder | [pka]
10.06±0.20(Predicted) | [color ]
white to beige |
| Hazard Information | Back Directory | [Uses]
UNC 0642 is an in vivo chemical probe of the lysine methyltransferases G9a and GLP which maintains high in vitro and cellular potency, low cell toxicity, and selectivity. | [Biochem/physiol Actions]
UNC0642 is a potent, selective inhibitor of histone methyltransferases G9a (EHMT2) and GLP (EHMT1), which catalyze the mono and dimethylation of lysine 9 of histone 3 (H3K9), and other non-histone substrates such as p53 and WIZ. UNC0642 has an in vitro IC50 <15 nM with greater than 100-fold selectivity over 13 other HMTs and selected representatives of kinases, ion channels, 7TMs, and other epigenetic proteins. UNC0642 has the same potency with improved PK properties relative to UNC0638, which should make it a more useful probe in an in vivo setting. For full characterization details, please visit the UNC0642 probe summary on the Structural Genomics Consortium (SGC) website.To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc | [in vivo]
A single intraperitoneal (IP) injection (5 mg/kg) of UNC0642 results in a plasma Cmax (maximum concentration) of 947 ng/mL and an AUC (area under the curve) of 1265 hr*ng/mL[1]. | [IC 50]
EHMT2/G9a/KMT1C; EHMT1/GLP/KMT1D | [storage]
Store at -20°C |
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| Company Name: |
Sigma-Aldrich
|
| Telephone: |
021-61415566 800-8193336 |
| Website: |
https://www.sigmaaldrich.cn |
| Company Name: |
SPIRO PHARMA
|
| Telephone: |
|
| Website: |
www.spiropharma.com.cn |
|