NSC 228155

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.

Product information

CAS Number: 113104-25-9

Molecular Weight: 290.25

Formula: C11H6N4O4S

Chemical Name: 2-[(7-nitro-2, 1, 3-benzoxadiazol-4-yl)sulfanyl]pyridin-1-ium-1-olate

Smiles: [O-][N+]1=CC=CC=C1SC1=CC=C(C2=NON=C12)[N+]([O-])=O

InChiKey: ICCFXXDUYSPKOL-UHFFFAOYSA-N

InChi: InChI=1S/C11H6N4O4S/c16-14-6-2-1-3-9(14)20-8-5-4-7(15(17)18)10-11(8)13-19-12-10/h1-6H

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 16 mg/mL (55.12 mM; Need ultrasonic)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

NSC 228155 (100 μM) enhances EGFR tyrosine phosphorylation via action of SOD1. 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. NSC 228155 is not selective against CREB-mediated gene transcription in living HEK 293T cells.

References:

1. Sakanyan V, et al. Activation of EGFR by small compounds through coupling the generation of hydrogen peroxide to stable dimerization of Cu/Zn SOD1. Sci Rep. 2016 Feb 17;6:21088.
2. Xie F, et al. 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.

Products are for research use only. Not for human use.