An activator of EGFR and an inhibitor of the interaction between the KID of CREB and the KIX domain of CBP (IC50 = 0.36 μM); increases phosphorylation of EGFR at Tyr1068 in MDA-MB-468 cells (EC50 = 52 μM)

NSC 228155 – 5 mg

Brand:
Cayman
CAS:
113104-25-9
Storage:
-20
UN-No:
Non-Hazardous - /

NSC 228155 is an activator of the EGF receptor (EGFR) and an inhibitor of the interaction between the kinase inducible domain (KID) of CREB and the KID-interacting (KIX) domain of CREB-binding protein (CBP; IC50 = 0.36 μM).{45576,45577} It increases phosphorylation of EGFR at Tyr1068 in MDA-MB-468 cells (EC50 = 52 μM), as well as phosphorylation of ERK1 and ERK2.{45576} NSC 228155 (100 μM) also induces transactivation of InsR, EphA1, ErbB2, ErbB3, IGF-1R, Mer, and ROR1 in MDA-MB-468 cells. It inhibits CREB-mediated transcription (IC50 = 2.09 μM), as well as transcription mediated by the constitutively active mutant VP16-CREB (IC50 = 6.14 μM), in HEK293T cell-based reporter assays.{45577} NSC 228155 also inhibits P. aeruginosa ribonucleotide reductase (IC50 = 26 μM) and is active against P. aeruginosa with an MIC value of 50 μM.{45578}  

 

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SKU: 28856 - 5 mg Category:

Description

An activator of EGFR and an inhibitor of the interaction between the KID of CREB and the KIX domain of CBP (IC50 = 0.36 μM); increases phosphorylation of EGFR at Tyr1068 in MDA-MB-468 cells (EC50 = 52 μM), as well as phosphorylation of ERK1 and ERK2; induces transactivation of InsR, EphA1, ErbB2, ErbB3, IGF-1R, Mer, and ROR1 in MDA-MB-468 cells at 100 μM; inhibits CREB- and VP16-CREB-mediated transcription in HEK293T cell-based reporter assays (IC50s = 2.09 and 6.14 μM, respectively); inhibits P. aeruginosa ribonucleotide reductase (IC50 = 26 μM) and is active against P. aeruginosa (MIC = 50 μM)

Formal name: 4-nitro-7-[(1-oxido-2-pyridinyl)thio]-2,1,3-benzoxadiazole

Synonyms: 

Molecular weight: 290.3

CAS: 113104-25-9

Purity: ≥98%

Formulation: A crystalline solid

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