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  2. Epigenetic Reader Domain
  3. KG-501

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

Cat. No.: HY-103299 Purity: 99.12%
Handling Instructions

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

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

KG-501 Chemical Structure

KG-501 Chemical Structure

CAS No. : 18228-17-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 55 In-stock
Estimated Time of Arrival: December 31
5 mg USD 50 In-stock
Estimated Time of Arrival: December 31
10 mg USD 70 In-stock
Estimated Time of Arrival: December 31
50 mg USD 160 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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 Ki 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].

Molecular Weight

377.72

Formula

C₁₇H₁₃ClNO₅P

CAS No.

18228-17-6

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)

H2O : < 0.1 mg/mL (insoluble)

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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2 mg/mL (5.29 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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KG-501
Cat. No.:
HY-103299
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