NAE-IN-M22-武汉科斯坦生物科技有限公司

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NAE-IN-M22

英文名称：NAE-IN-M22

品牌：Chemstan

产地：中国

货号：CS-115537

cas：864420-54-2

价格： ￥4000/mg
发布日期： 2021-03-10
更新日期： 2025-09-19

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产品详请

产地	中国
品牌	Chemstan
货号	CS-115537
用途	科研
英文名称	NAE-IN-M22
包装规格	5 mg
纯度	98.00%%
CAS编号	864420-54-2
别名
分子式
是否进口	否

Description

NAE-IN-M22 is a potent, selective and reversible inhibitor of NEDD8 activating enzyme (NAE), with potency in micromolar range. NAE-IN-M22 inhibits multiple cancer cell lines and induces apoptosis in A549 cells. NAE-IN-M22 also can inhibit tumor growth in vivo^[1].

IC₅₀ & Target

NEDD8 activating enzyme (NAE)^[1]

In Vitro

M22 (0.37-90 μM; 24 h) blocks neddylation pathway selectively and suppresses degradation of CRL substrates in A549 cells^[1].
M22 (0.1-100 μM; 48 h) inhibits A549 cell proliferation completely at 30 μM (GI₅₀=5.5 μM, GI₉₀=19.3 μM)^[1].
M22 (15-30 μM; 36 h) promotes apoptosis in A549 cell line^[1].

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

Cell Viability Assay^[1]

Cell Line:	A549 cells
Concentration:	0.37, 1.11, 3.33, 10, 30, 90 μM
Incubation Time:	24 hours
Result:	Inhibited formations of Uba3-NEDD8 and Ubc12-NEDD8. Resulted in a corresponding decrease in the abundance of Cullins-NEDD8. Decreased the degradations of p27 and CDT1. Prevented p53 from degradation.

In Vivo

M22 (60 mg/kg; i.p. once daily for 14 d) inhibits tumor growth in nude mice bearing AGS xenografts^[1].
M22 (0.36-90 μM) has low acute toxicity in zebrafish model^[1].

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

Molecular Weight

363.32

Formula

C??H??Cl?N?

CAS No.

864420-54-2

SMILES

ClC1=CC=C(CCNC2CCN(CC3=CC=CC=C3)CC2)C(Cl)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMSO : 250 mg/mL (688.10 mM; Need ultrasonic)

Preparing
Stock Solutions

ConcentrationSolventMass	1 mg	5 mg	10 mg

1 mM	2.7524 mL	13.7620 mL	27.5239 mL
5 mM	0.5505 mL	2.7524 mL	5.5048 mL
10 mM	0.2752 mL	1.3762 mL	2.7524 mL

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。

In Vivo:

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: ≥ 2.08 mg/mL (5.72 mM); Clear solution
2.

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

Solubility: ≥ 2.08 mg/mL (5.72 mM); Clear solution
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.08 mg/mL (5.72 mM); Clear solution

*以上所有助溶剂都可在 MCE 网站选购。

References

[1]. Lu P, et, al. Discovery of a novel NEDD8 Activating Enzyme Inhibitor with Piperidin-4-amine Scaffold by Structure-Based Virtual Screening. ACS Chem Biol. 2016 Jul 15;11(7):1901-7.