NSC228155 |
Catalog No.GC14103
One-Click Copy Product Info
|
EGFR activator
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 113104-25-9
Sample solution is provided at 25 µL, 10mM.
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IC50: 0.36 μM for KIX-KID interaction
NSC228155 is a potent inhibitor of KIX-KID interaction.
Cyclic-AMP response-element binding protein (CREB) is identified as a stimulus-activated transcription factor. Its transcription activity needs its binding with CREB-binding protein (CBP) after CREB is phosphorylated at Ser133. The domains involved for CREB-CBP interaction are kinase-inducible domain (KID) from CREB and KID-interacting domain (KIX) from CBP.
In vitro: Previous study found that NSC228155 could dose-dependently inhibit KIX–KID interaction as measured by the split RLuc assay. In living HEK 293T cells, NSC228155 could inhibit CREB-mediated gene transcription with an IC50 of 2.09 μM. NSC228155 also inhibited VP16-CREB-mediated gene transcription with an IC50 of 6.14 μM. Though this was around 3-fold higher than the IC50 of CREB-mediated gene transcription, such results indicated that NSC228155 was not particularly selective in inhibiting KIX–KID interaction inside these living cells. Therefore, although NSC228155 was a potent inhibitor of KIX-KID interaction, it was not selective against CREB-mediated gene transcription, and further SAR studies identified a 4-aniline substituted analog displaying a higher selectivity index [1].
In vivo: So far, there is no animal in vivo data reported.
Clinical trial: Up to now, NSC228155 is still in the preclinical development stage.
Reference:
[1] Xie F, Li BX, Broussard C, Xiao X. Identification, synthesis and evaluation of substituted benzofurazans as inhibitors of CREB-mediated gene transcription. Bioorg Med Chem Lett. 2013 Oct 1;23(19):5371-5.
| Cas No. | 113104-25-9 | SDF | |
| Chemical Name | 2-((7-nitrobenzo[c][1,2,5]oxadiazol-4-yl)thio)pyridine 1-oxide | ||
| Canonical SMILES | [O-][N+]1=CC=CC=C1SC2=CC=C([N+]([O-])=O)C3=NON=C32 | ||
| Formula | C11H6N4O4S | M.Wt | 290.25 |
| Solubility | ≥ 29mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.4453 mL | 17.2265 mL | 34.4531 mL |
| 5 mM | 689.1 μL | 3.4453 mL | 6.8906 mL |
| 10 mM | 344.5 μL | 1.7227 mL | 3.4453 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)