NSC228155 | CAS#113104-25-9 | KIX-KID inhibitor

MedKoo Cat#: 563342 | Name: NSC228155

Description:

WARNING: This product is for research use only, not for human or veterinary use.

NSC228155 is an inhibitor of KIX-KID interaction that acts by enhancing tyrosine phosphorylation of EGFR.

Chemical Structure

NSC228155

CAS#113104-25-9

Theoretical Analysis

MedKoo Cat#: 563342

Name: NSC228155

CAS#: 113104-25-9

Chemical Formula: C11H6N4O4S

Exact Mass: 290.0110

Molecular Weight: 290.25

Elemental Analysis: C, 45.52; H, 2.08; N, 19.30; O, 22.05; S, 11.05

Price and Availability

Size	Price	Availability
100mg	USD 850.00	2 Weeks
200mg	USD 1,450.00	2 Weeks
500mg	USD 2,150.00	2 Weeks
1g	USD 2,950.00	2 Weeks
2g	USD 5,450.00	2 Weeks

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Related CAS #

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Synonym

NSC228155; NSC-228155; NSC 228155;

IUPAC/Chemical Name

2-[(7-Nitrobenzo[c][1,2,5]oxadiazol-4-yl)thio]pyridine 1-oxide

InChi Key

ICCFXXDUYSPKOL-UHFFFAOYSA-N

InChi Code

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

SMILES Code

O=[N+](C1=CC=C(SC2=CC=CC=[N+]2[O-])C3=NON=C31)[O-]

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>3 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.03.00

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

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.

In vitro activity:

The data presented in Figure 2B and Table 1 showed that compound 1 inhibited CREB-mediated gene transcription in living HEK 293T cells with an IC50 of 2.09 μM. To investigate if the inhibition of the CREB's transcription activity by compound 1 was dependent on KIX-KID interaction, another transcription reporter assay activated by a heterologous transcription activator, VP16-CREB, was performed in HEK 293T cells. Reference: Bioorg Med Chem Lett. 2013 Oct 1;23(19):5371-5. https://pubmed.ncbi.nlm.nih.gov/23953193/

In vivo activity:

NSC228155 significantly improved cardiac function examined by echocardiography, decreased the serum lactate dehydrogenase (LDH) and creatine kinase-MB, and pathologically alleviated cardiac injury in LPS mice. Accordingly, NSC228155 attenuated cardiomyocytes' mitochondrial damage as shown by decreased damaged mitochondrial ratio and activated signals for mitochondrial biogenesis, dynamics and mitophagy in LPS mice model. Metabolomics analysis demonstrated that NSC228155 corrected the metabolic disturbance involved in oxidative stress and energy metabolism, and decreased tissue injury metabolites in LPS-stimulated cardiac tissue. Reference: Int Immunopharmacol. 2023 Mar;116:109847. https://pubmed.ncbi.nlm.nih.gov/36774857/

	Solvent	mg/mL	mM
Solubility
	DMF	10.0	34.45
	DMSO	28.0	96.47
	DMSO:PBS (pH 7.2) (1:9)	0.1	0.34

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 290.25 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Jiang Y, Li Y, Zhang Y, Hu D, Zhang S, Wang C, Huang S, Zhang A, Jia Z, You R. NSC228155 alleviates septic cardiomyopathy via protecting mitochondria and inhibiting inflammation. Int Immunopharmacol. 2023 Mar;116:109847. doi: 10.1016/j.intimp.2023.109847. Epub 2023 Feb 10. PMID: 36774857. 2. 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. doi: 10.1016/j.bmcl.2013.07.053. Epub 2013 Jul 31. PMID: 23953193; PMCID: PMC3783659. 3. Li Y, Jiang Y, Zhou W, Wu Y, Zhang S, Ding G, Zhang Y, Zhang A, Huang S, Jia Z, You R. Maintaining homeostasis of mitochondria and endoplasmic reticulum with NSC228155 alleviates cisplatin-induced acute kidney injury. Free Radic Biol Med. 2022 Mar;181:270-287. doi: 10.1016/j.freeradbiomed.2022.02.003. Epub 2022 Feb 5. PMID: 35134531.

In vitro protocol:

In vivo protocol:

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. doi: 10.1016/j.bmcl.2013.07.053. Epub 2013 Jul 31. PubMed PMID: 23953193; PubMed Central PMCID: PMC3783659.