2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Epigenetics
  3. EGFR Histone Acetyltransferase Epigenetic Reader Domain
  4. NSC 228155

NSC 228155 est un activateur de EGFR, se lie à la région extracellulaire de EGFR et améliore la phosphorylation de la tyrosine d'EGFR. NSC 228155 est également un inhibiteur puissant de l'interaction KIX-KID, inhibe le domaine inductible par kinase (KID) de CREB et le domaine interagissant avec KID (KIX) de CBP, avec un IC50 de 0,36 μM.

NSC 228155 is an activator of EGFR, binds to the extracellular region of EGFR and enhance tyrosine phosphorylation of EGFR. NSC 228155 is also a potent inhibitor of KIX-KID interaction, inhibits kinase-inducible domain (KID) from CREB and KID-interacting domain (KIX) from CBP, with an IC50 of 0.36 μM.

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NSC 228155 Chemical Structure

NSC 228155 Chemical Structure

CAS No. : 113104-25-9

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Customer Review

Based on 10 publication(s) in Google Scholar

NSC 228155 Related Antibodies

Top Publications Citing Use of Products

View All EGFR Isoform Specific Products:

View All Isoforms
EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

View All Histone Acetyltransferase Isoform Specific Products:

View All Isoforms
CBP/p300 GCN5/PCAF TIP60 MOZ/MORF HBO1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

NSC 228155 is an activator of EGFR, binds to the extracellular region of EGFR and enhance tyrosine phosphorylation of EGFR[1]. NSC 228155 is also a potent inhibitor of KIX-KID interaction, inhibits kinase-inducible domain (KID) from CREB and KID-interacting domain (KIX) from CBP, with an IC50 of 0.36 μM[2].

IC50 & Target[1][2]

CBP/p300

 

EGFR

 

KIX-KID

0.36 μM (IC50)

Cellular Effect
Cell Line Type Value Description References
HEK-293T IC50
2.09 μM
Compound: 1, NSC228155
Inhibition of CREB (unknown origin)-mediated gene transcription in HEK293T cells preincubated for 30 mins followed by forskolin addition measured after 5 hrs by luciferase reporter gene assay
Inhibition of CREB (unknown origin)-mediated gene transcription in HEK293T cells preincubated for 30 mins followed by forskolin addition measured after 5 hrs by luciferase reporter gene assay
[PMID: 23953193]
HEK-293T IC50
6.14 μM
Compound: 1, NSC228155
Inhibition of Herpesvirus VP16-CREB (unknown origin)-mediated gene transcription in HEK293T cells by luciferase reporter gene assay
Inhibition of Herpesvirus VP16-CREB (unknown origin)-mediated gene transcription in HEK293T cells by luciferase reporter gene assay
[PMID: 23953193]
In Vitro

NSC 228155 (100 μM) enhances EGFR tyrosine phosphorylation via the action of SOD1[1].
NSC 228155 (Compound 1) inhibits CREB- and VP16-CREB-mediated gene transcription in living HEK 293T cells with IC50s of 2.09 and 6.14 μM, respectively[2].
NSC 228155 is not selective against CREB-mediated gene transcription in living HEK 293T cells[2].

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

NSC 228155 Related Antibodies
Molecular Weight

290.25

Formula

C11H6N4O4S
CAS No.
Appearance

Solid

Color

Light yellow to orange

SMILES

[O-][N+]1=CC=CC=C1SC2=CC=C([N+]([O-])=O)C3=NON=C32
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
Solvent & Solubility
In Vitro: 

DMSO : 16 mg/mL (55.12 mM; Need ultrasonic; 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 3.4453 mL 17.2265 mL 34.4531 mL
5 mM 0.6891 mL 3.4453 mL 6.8906 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

  • Molarity Calculator

  • Dilution Calculator

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

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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

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    90% Corn Oil

    Solubility: ≥ 1.6 mg/mL (5.51 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.6 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 (16.0 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  15% Cremophor EL    85% Saline

    Solubility: 2 mg/mL (6.89 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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 +
%
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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
References

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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.4453 mL 17.2265 mL 34.4531 mL 86.1326 mL
5 mM 0.6891 mL 3.4453 mL 6.8906 mL 17.2265 mL
10 mM 0.3445 mL 1.7227 mL 3.4453 mL 8.6133 mL
15 mM 0.2297 mL 1.1484 mL 2.2969 mL 5.7422 mL
20 mM 0.1723 mL 0.8613 mL 1.7227 mL 4.3066 mL
25 mM 0.1378 mL 0.6891 mL 1.3781 mL 3.4453 mL
30 mM 0.1148 mL 0.5742 mL 1.1484 mL 2.8711 mL
40 mM 0.0861 mL 0.4307 mL 0.8613 mL 2.1533 mL
50 mM 0.0689 mL 0.3445 mL 0.6891 mL 1.7227 mL
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NSC 228155 Related Classifications

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:

NSC 228155113104-25-9NSC228155NSC-228155EGFRHistone AcetyltransferaseEpigenetic Reader DomainEpidermal growth factor receptorErbB-1HER1HATsHATInhibitorinhibitorinhibit

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