nAS-E | CAS# 92-78-4 | KIX-KID Inhibitor

MedKoo Cat#: 565338 | Name: nAS-E

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

nAS-E is an inhibitor of the KIX-KID interaction and CREB-mediated gene transcription.

Chemical Structure

nAS-E

CAS#92-78-4

Theoretical Analysis

MedKoo Cat#: 565338

Name: nAS-E

CAS#: 92-78-4

Chemical Formula: C17H12ClNO2

Exact Mass: 297.0557

Molecular Weight: 297.74

Elemental Analysis: C, 68.58; H, 4.06; Cl, 11.91; N, 4.70; O, 10.75

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Synonym

Naphthol AS-E; nAS-E; nAS E

IUPAC/Chemical Name

N-(4-Chlorophenyl)-3-hydroxy-2-naphthamide

InChi Key

OHAXNCGNVGGWSO-UHFFFAOYSA-N

InChi Code

InChI=1S/C17H12ClNO2/c18-13-5-7-14(8-6-13)19-17(21)15-9-11-3-1-2-4-12(11)10-16(15)20/h1-10,20H,(H,19,21)

SMILES Code

O=C(NC1=CC=C(Cl)C=C1)C2=C(O)C=C3C=CC=CC3=C2

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>3 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

Naphthol AS-E is a potent and cell-permeable inhibitor of KIX-KID interaction.

In vitro activity:

This study describes the discovery of naphthol AS-E (1) as a cell-permeable small-molecule inhibitor of the KIX–KID interaction by using a novel Renilla luciferase complementation assay. Reference: Chembiochem. 2009 Nov 23;10(17):2721-4. https://pubmed.ncbi.nlm.nih.gov/19810079/

In vivo activity:

In addition, the in vivo effect of nAS-E in protecting against breast cancer-induced osteolysis was evaluated in mice. These results indicated that nAS-E could reverse bone loss induced by MDA-MB-231 tumour. Reference: J Cell Mol Med. 2019 Feb;23(2):1224-1234. https://pubmed.ncbi.nlm.nih.gov/30461194/

	Solvent	mg/mL	mM	comments
Solubility
	DMSO	41.7	139.96

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 297.74 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Yang Q, Tang J, Cao J, Liu F, Fu M, Xue B, Zhou A, Chen S, Liu J, Zhou Y, Shi Y, Peng W, Chen X. SARS-CoV-2 infection activates CREB/CBP in cellular cyclic AMP-dependent pathways. J Med Virol. 2023 Jan;95(1):e28383. doi: 10.1002/jmv.28383. PMID: 36477795; PMCID: PMC9877775. 2. Li BX, Xiao X. Discovery of a small-molecule inhibitor of the KIX-KID interaction. Chembiochem. 2009 Nov 23;10(17):2721-4. doi: 10.1002/cbic.200900552. PMID: 19810079; PMCID: PMC4214275. 3. Kuang Q, Liang Y, Zhuo Y, Cai Z, Jiang F, Xie J, Zheng Y, Zhong W. The ALDOA Metabolism Pathway as a Potential Target for Regulation of Prostate Cancer Proliferation. Onco Targets Ther. 2021 May 24;14:3353-3366. doi: 10.2147/OTT.S290284. PMID: 34079281; PMCID: PMC8163754. 4. Jiang M, Yan Y, Yang K, Liu Z, Qi J, Zhou H, Qian N, Zhou Q, Wang T, Xu X, Xiao X, Deng L. Small molecule nAS-E targeting cAMP response element binding protein (CREB) and CREB-binding protein interaction inhibits breast cancer bone metastasis. J Cell Mol Med. 2019 Feb;23(2):1224-1234. doi: 10.1111/jcmm.14024. Epub 2018 Nov 20. PMID: 30461194; PMCID: PMC6349349.

In vitro protocol:

In vivo protocol:

1. Kuang Q, Liang Y, Zhuo Y, Cai Z, Jiang F, Xie J, Zheng Y, Zhong W. The ALDOA Metabolism Pathway as a Potential Target for Regulation of Prostate Cancer Proliferation. Onco Targets Ther. 2021 May 24;14:3353-3366. doi: 10.2147/OTT.S290284. PMID: 34079281; PMCID: PMC8163754. 2. Jiang M, Yan Y, Yang K, Liu Z, Qi J, Zhou H, Qian N, Zhou Q, Wang T, Xu X, Xiao X, Deng L. Small molecule nAS-E targeting cAMP response element binding protein (CREB) and CREB-binding protein interaction inhibits breast cancer bone metastasis. J Cell Mol Med. 2019 Feb;23(2):1224-1234. doi: 10.1111/jcmm.14024. Epub 2018 Nov 20. PMID: 30461194; PMCID: PMC6349349.

1: Jiang M, Yan Y, Yang K, Liu Z, Qi J, Zhou H, Qian N, Zhou Q, Wang T, Xu X, Xiao X, Deng L. Small molecule nAS-E targeting cAMP response element binding protein (CREB) and CREB-binding protein interaction inhibits breast cancer bone metastasis. J Cell Mol Med. 2019 Feb;23(2):1224-1234. doi: 10.1111/jcmm.14024. Epub 2018 Nov 20. PubMed PMID: 30461194; PubMed Central PMCID: PMC6349349.