UNC0642是有效，选择性的赖氨酸甲基转移酶 G9a 和

UNC0642 is a potent and selective lysine methyltransferases G9a and GLP inhibitor, with an IC₅₀ of <2.5 nM for G9a.

IC50: <2.5 nM (G9a)^[1]

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 K_i 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

A single intraperitoneal (IP) injection (5 mg/kg) of UNC0642 results in a plasma C_max (maximum concentration) of 947 ng/mL and an AUC (area under the curve) of 1265 hr*ng/mL^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

546.70

Solid

C₂₉H₄₄F₂N₆O₂

1481677-78-4

Room temperature in continental US; may vary elsewhere.

DMSO : 50 mg/mL (91.46 mM; Need ultrasonic)

H₂O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

  Solubility: ≥ 2.5 mg/mL (4.57 mM); Clear solution

• 2.

  请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

  Solubility: ≥ 2.5 mg/mL (4.57 mM); Clear solution

• 3.

  请依序添加每种溶剂： 10% DMSO 90% corn oil

  Solubility: ≥ 2.5 mg/mL (4.57 mM); Clear solution