Synonym
SR-12460; SR 12460; SR12460
IUPAC/Chemical Name
2-((5-Chloropyridin-2-yl)amino)-N-(3,5-difluorophenethyl)acetamide
InChi Key
XNEWRBBKUMGNPC-UHFFFAOYSA-N
InChi Code
InChI=1S/C15H14ClF2N3O/c16-11-1-2-14(20-8-11)21-9-15(22)19-4-3-10-5-12(17)7-13(18)6-10/h1-2,5-8H,3-4,9H2,(H,19,22)(H,20,21)
SMILES Code
O=C(NCCC1=CC(F)=CC(F)=C1)CNC2=NC=C(Cl)C=C2
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
Biological target:
SR12460 is a mimetic of the IκB kinase β (IKKβ) NEMO/IKKγ-binding domain (NBD) that inhibits the protein-protein interaction between the IKK complex subunits NF-κB essential modulator (NEMO/IKKγ) and IKKβ.
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 |
comments |
| Solubility |
| DMF |
30.0 |
92.10 |
|
| DMSO |
15.0 |
46.05 |
|
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
325.74
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. 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 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.
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. eCollection 2018 Jun. PubMed PMID: 29889904; PubMed Central PMCID: PMC6013238.
