KG-501 (Synonyms: Naphthol AS-E phosphate)

Name: KG-501
Brand: MedChemExpress
SKU: HY-103299
Rating: 5.0 (21 reviews)

Cat. No.: HY-103299 Purity: 99.45%: Data Sheet
COA

SDS
Handling Instructions
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Technical Support

KG-501 is a CREB inhibitor, with an IC₅₀ of 6.89 μM.

For research use only. We do not sell to patients.

CAS No. : 18228-17-6

Size	Stock	Quantity

Free Sample (0.1 - 0.2 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	Get quote
200 mg	Get quote

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Customer Review

Based on 21 publication(s) in Google Scholar

Other Forms of KG-501:

KG-501 (Standard) Get quote

21 Publications Citing Use of MCE KG-501

Flow Cytometry

Bio/Physico-chemical Assay

Cell Imaging/Staining

RT-PCR

: KG-501 purchased from MedChemExpress. Usage Cited in: Environ Sci Technol. 2025 Sep 30;59(38):20263-20275. [Abstract]; KG-501 (156.25, 312.5, 625, 1250, 2500, 5000, 10000 nM) inhibited CREB transcriptional activity, as measured by a dual-luciferase reporter assay in HEK-293T cells.

: KG-501 purchased from MedChemExpress. Usage Cited in: Environ Sci Technol. 2025 Sep 30;59(38):20263-20275. [Abstract]; KG-501 (500 nM; 7 days) decreased the CYP19A1 mRNA expression in human trophoblast organoids.

: KG-501 purchased from MedChemExpress. Usage Cited in: Environ Sci Technol. 2025 Sep 30;59(38):20263-20275. [Abstract]; KG-501 (500 nM; 7 days) decreased the STB marker SDC-1 in human trophoblast organoids.

: KG-501 purchased from MedChemExpress. Usage Cited in: Environ Sci Technol. 2025 Sep 30;59(38):20263-20275. [Abstract]; Representative images of the fusion assay of trophoblast organoids stained for F-actin and DAPI treated with KG-501 (500 nM; 7 days).

: KG-501 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2024 Aug 20;43(1):233. [Abstract]; KG-501 (300 μM; 1 h) suppressed surface expression of CXCR4, maturation/activation marker including CD10, CD101, degranulation marker CD63 in CXCR4^hi neutrophils.

: KG-501 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2024 Aug 20;43(1):233. [Abstract]; Representative co-staining of DNA (Hoechst), Cit-H3 (citrullinated histone-3, red), and MPO (myeloperoxidase, green) to assess NETs formation in psoriatic neutrophils in vitro after pretreatment with KG-501 (300 μM) for 1 h. Scale bar = 20 µm

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Description

KG-501 is a CREB inhibitor, with an IC₅₀ of 6.89 μM.

IC₅₀ & Target

IC50: 6.89 μM (CREB)^[1].

In Vitro

KG-501, which directly targets the KIX domain of CBP, results in a disrupted CREB-CBP complex, inhibits CREB-target gene induction, and inhibits IL-1β-mediated angiogenic activity in NSCLC^[1]. KG-501 disrupts phospho (Ser-133) CREB binding to KIX with a K_i of ~90 μM, using concentrations of CREB that are within the linear range of the binding assay. Treatment of HEK293T cells with KG-501 also blocks induction of endogenous CREB target genes (NR4A2, αCG, c-fos, and RGS2) by forskolin, indicating that KG-501 likely exerts a general effect on CREB activity^[2]. KG-501 can also inhibit NF-κB transcription activity because NF-κB also uses CBP as a cofactor to regulate gene expression. The migration of HUVECs induced by CM from A549 cells treated with IL-1β plus 10 μM of KG-501 is significantly lower than that induced by CM from A549 cells treated with IL-1β alone. At 10 μM, KG-501 suppresses the expression of all of the IL-1β–induced CXC chemokine genes except CXCL8. For the protein level, KG-501 significantly suppresses IL-1β–induced CXCL5 protein secretion. Similar effects of KG-501 are also observed in the H1734 cell line^[3].

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

Molecular Weight

377.72

Formula

C₁₇H₁₃ClNO₅P

CAS No.

18228-17-6

Appearance

Solid

Color

White to light yellow

SMILES

O=C(C1=C(OP(O)(O)=O)C=C2C=CC=CC2=C1)NC3=CC=C(Cl)C=C3

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 : 6 mg/mL (15.88 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.6475 mL	13.2373 mL	26.4746 mL
5 mM	0.5295 mL	2.6475 mL	5.2949 mL
10 mM	0.2647 mL	1.3237 mL	2.6475 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2 mg/mL (5.29 mM); Clear solution

This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2 mg/mL (5.29 mM); Suspended solution

This protocol yields a suspended solution of ≥ 2 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2 mg/mL (5.29 mM); Clear solution

This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.45%

Select Batch:

Data Sheet (278 KB) SDS (396 KB)

COA (252 KB) RP-HPLC (223 KB) MS (68 KB)

Handling Instructions (2659 KB)

References

[1]. Lee JW, et al. A Novel Small-Molecule Inhibitor Targeting CREB-CBP Complex Possesses Anti-Cancer Effects along with Cell Cycle Regulation, Autophagy Suppression and Endoplasmic Reticulum Stress. PLoS One. 2015 Apr 21;10(4):e0122628. [Content Brief]

[2]. Best JL et al. Identification of small-molecule antagonists that inhibit an activator: coactivator interaction. Proc Natl Acad Sci U S A. 2004 Dec 21;101(51):17622-7 [Content Brief]

[3]. Sun H, et al. Cyclic AMP-responsive element binding protein- and nuclear factor-kappaB-regulated CXC chemokine gene expression in lung carcinogenesis. Cancer Prev Res (Phila). 2008 Oct;1(5):316-28. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.6475 mL	13.2373 mL	26.4746 mL	66.1866 mL
	5 mM	0.5295 mL	2.6475 mL	5.2949 mL	13.2373 mL
	10 mM	0.2647 mL	1.3237 mL	2.6475 mL	6.6187 mL
	15 mM	0.1765 mL	0.8825 mL	1.7650 mL	4.4124 mL

KG-501 Related Classifications

Inflammation/Immunology

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

KG-50118228-17-6Naphthol AS-EKG501KG 501Epigenetic Reader DomainInhibitorinhibitorinhibit

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KG-501 (Synonyms: Naphthol AS-E phosphate)

Customer Review

Other Forms of KG-501:

KG-501 Related Antibodies

21 Publications Citing Use of MCE KG-501

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Purity & Documentation

References

Customer Review

KG-501 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

KG-501 Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

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