Synonym
MS-1020; MS 1020; MS1020
IUPAC/Chemical Name
1-Hydroxy-N-[2-(5-hydroxy-1H-indol-3-yl)ethyl]-2-naphthalenecarboxamide
InChi Key
KHJNISGKGIHTMY-UHFFFAOYSA-N
InChi Code
InChI=1S/C21H18N2O3/c24-15-6-8-19-18(11-15)14(12-23-19)9-10-22-21(26)17-7-5-13-3-1-2-4-16(13)20(17)25/h1-8,11-12,23-25H,9-10H2,(H,22,26)
SMILES Code
O=C(C1=CC=C2C=CC=CC2=C1O)NCCC3=CNC4=C3C=C(O)C=C4
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
>2 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
2934.99.9001
Biological target:
MS-1020 is a potent and ATP-competitive JAK3 inhibitor.
In vitro activity:
MS-1020 potently inhibited persistently-active STAT3 in a cell type-specific manner. Further examination showed that MS-1020 selectively blocked constitutively-active JAK3 and consistently suppressed interleukin-2-induced JAK3/STAT5 signalling but not prolactin-induced JAK2/STAT5 signalling. Furthermore, MS-1020 affected cell viability only in cancer cells harbouring persistently-active JAK3/STATs, and in vitro kinase assays showed MS-1020 binds directly with JAK3, blocking its catalytic activity.
Reference: Br J Haematol. 2010 Jan;148(1):132-43. https://pubmed.ncbi.nlm.nih.gov/19793252/
Preparing Stock Solutions
The following data is based on the
product
molecular weight
346.39
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:
Kim BH, Oh SR, Yin CH, Lee S, Kim EA, Kim MS, Sandoval C, Jayabose S, Bach EA, Lee HK, Baeg GH. MS-1020 is a novel small molecule that selectively inhibits JAK3 activity. Br J Haematol. 2010 Jan;148(1):132-43. doi: 10.1111/j.1365-2141.2009.07925.x. Epub 2009 Sep 29. PMID: 19793252; PMCID: PMC3034357.
In vitro protocol:
Kim BH, Oh SR, Yin CH, Lee S, Kim EA, Kim MS, Sandoval C, Jayabose S, Bach EA, Lee HK, Baeg GH. MS-1020 is a novel small molecule that selectively inhibits JAK3 activity. Br J Haematol. 2010 Jan;148(1):132-43. doi: 10.1111/j.1365-2141.2009.07925.x. Epub 2009 Sep 29. PMID: 19793252; PMCID: PMC3034357.
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7: Kurosawa M, Messlinger K, Pawlak M, Schmidt RF. Increase of meningeal blood flow after electrical stimulation of rat dura mater encephali: mediation by calcitonin gene-related peptide. Br J Pharmacol. 1995 Apr;114(7):1397-402. PubMed PMID: 7606344; PubMed Central PMCID: PMC1510285.
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