NAE-IN-M22


Catalog No. Size PriceQuantity
M13358-2 2mg solid $365
M13358-10 10mg solid $1,460

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.

Product information

CAS Number: 864420-54-2

Molecular Weight: 363.32

Formula: C20H24Cl2N2

Chemical Name: 1-benzyl-N-[2-(2,4-dichlorophenyl)ethyl]piperidin-4-amine

Smiles: ClC1C=C(Cl)C(CCNC2CCN(CC3C=CC=CC=3)CC2)=CC=1

InChiKey: WMEXQHGRMWPOEF-UHFFFAOYSA-N

InChi: InChI=1S/C20H24Cl2N2/c21-18-7-6-17(20(22)14-18)8-11-23-19-9-12-24(13-10-19)15-16-4-2-1-3-5-16/h1-7,14,19,23H,8-13,15H2

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

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

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

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

In Vivo:

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

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.

Products are for research use only. Not for human use.

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