SR12343 | CAS#2055101-86-3 | IKKβ/NEMO Blocker

MedKoo Cat#: 564656 | Name: SR12343

Featured

Description:

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

SR12343 is an inhibitor of tumor necrosis factor α (TNF-α)- and lipopolysaccharide (LPS)-induced NF-κB activation by blocking the interaction between IKKβ and NEMO, suppressing LPS-induced acute pulmonary inflammation in mice.

Chemical Structure

SR12343

CAS#2055101-86-3

Theoretical Analysis

MedKoo Cat#: 564656

Name: SR12343

CAS#: 2055101-86-3

Chemical Formula: C15H15BrClN3O

Exact Mass: 367.0087

Molecular Weight: 368.66

Elemental Analysis: C, 48.87; H, 4.10; Br, 21.67; Cl, 9.62; N, 11.40; O, 4.34

Price and Availability

Size	Price	Availability
1mg	USD 220.00	2 Weeks
5mg	USD 390.00	2 Weeks
10mg	USD 630.00	2 Weeks

Bulk Inquiry

Buy Now

Add to Cart

Related CAS #

No Data

Synonym

SR-12343; SR 12343; SR12343

IUPAC/Chemical Name

N-(3-Bromophenethyl)-2-((5-chloropyridin-2-yl)amino)acetamide

InChi Key

PEOFCAIUELALCR-UHFFFAOYSA-N

InChi Code

InChI=1S/C15H15BrClN3O/c16-12-3-1-2-11(8-12)6-7-18-15(21)10-20-14-5-4-13(17)9-19-14/h1-5,8-9H,6-7,10H2,(H,18,21)(H,19,20)

SMILES Code

O=C(NCCC1=CC=CC(Br)=C1)CNC2=NC=C(Cl)C=C2

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:

SR12343 inhibits the protein-protein interaction between the IKK complex subunits NF-κB essential modulator (NEMO/IKKγ) and IKKβ. It selectively disrupts the association of NEMO/IKKγ with IKKβ over TNF receptor-associated factor 2 (TRAF2), IκBα, and IKKα in co-immunoprecipitation assays using RAW 264.7 cells at concentrations ranging from 25 to 150 µM.

In vitro activity:

To be determined

In vivo activity:

NF-κB essential modulator (NEMO)-binding domain (NBD) mimetics have potential in inflammatory and degenerative disease treatments. SR12343 and SR12460 inhibited TNF-α- and LPS-induced NF-κB activation by blocking the interaction between IKKβ and NEMO and suppressed LPS-induced acute pulmonary inflammation in mice. In a mouse model of Duchenne muscular dystrophy, chronic treatment with SR12343 and SR12460 attenuated inflammatory infiltration, necrosis and muscle degeneration. Reference: PLoS Biol. 2018 Jun 11;16(6):e2004663. https://pubmed.ncbi.nlm.nih.gov/29889904/

	Solvent	mg/mL	mM
Solubility
	DMSO	30.0	81.37
	DMF	30.0	81.37
	Ethanol	30.0	81.37

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 368.66 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. Zhang L, Zhao J, Mu X, McGowan SJ, Angelini L, O'Kelly RD, Yousefzadeh MJ, Sakamoto A, Aversa Z, LeBrasseur NK, Suh Y, Huard J, Kamenecka TM, Niedernhofer LJ, Robbins PD. Novel small molecule inhibition of IKK/NF-κB activation reduces markers of senescence and improves healthspan in mouse models of aging. Aging Cell. 2021 Dec;20(12):e13486. doi: 10.1111/acel.13486. Epub 2021 Nov 3. PMID: 34734460; PMCID: PMC8672781. 2. Zhao J, Zhang L, Mu X, Doebelin C, Nguyen W, Wallace C, Reay DP, McGowan SJ, Corbo L, Clemens PR, Wilson GM, Watkins SC, Solt LA, Cameron MD, Huard J, Niedernhofer LJ, Kamenecka TM, Robbins PD. Development of novel NEMO-binding domain mimetics for inhibiting IKK/NF-κB activation. PLoS Biol. 2018 Jun 11;16(6):e2004663. doi: 10.1371/journal.pbio.2004663. PMID: 29889904; PMCID: PMC6013238.

In vitro protocol:

To be determined

In vivo protocol:

1:Zhao J, Zhang L, Mu X, Doebelin C, Nguyen W, Wallace C, Reay DP, McGowan SJ, Corbo L, Clemens PR, Wilson GM, Watkins SC, Solt LA, Cameron MD, Huard J, Niedernhofer LJ, Kamenecka TM, Robbins PD. Development of novel NEMO-binding domain mimetics for inhibiting IKK/NF-κB activation. PLoS Biol. 2018 Jun 11;16(6):e2004663. doi: 10.1371/journal.pbio.2004663. PMID: 29889904; PMCID: PMC6013238. 2: Zhao J, Zhang L, Mu X, Doebelin C, Nguyen W, Wallace C, Reay DP, McGowan SJ, Corbo L, Clemens PR, Wilson GM, Watkins SC, Solt LA, Cameron MD, Huard J, Niedernhofer LJ, Kamenecka TM, Robbins PD. Development of novel NEMO-binding domain mimetics for inhibiting IKK/NF-κB activation. PLoS Biol. 2018 Jun 11;16(6):e2004663. doi: 10.1371/journal.pbio.2004663. eCollection 2018 Jun. PubMed PMID: 29889904; PubMed Central PMCID: PMC6013238. 3: Englund DA, Jolliffe AM, Hanson GJ, Aversa Z, Zhang X, Jiang X, White TA, Zhang L, Monroe DG, Robbins PD, Niedernhofer LJ, Kamenecka TM, Khosla S, LeBrasseur NK. Senotherapeutic drug treatment ameliorates chemotherapy-induced cachexia. JCI Insight. 2024 Jan 23;9(2):e169512. doi: 10.1172/jci.insight.169512. PMID: 38051584; PMCID: PMC10906225.

View History

SR-32229

MedKoo CAT#: 130270

CAS#: N/A