ML-9A selective inhibitor of MYLK, CaMK, PKB Kinase, PKA, and Stim1

ML-9 (CAS 105637-50-1)

ML-9 | CAS 105637-50-1 is rated 5.0 out of 5 by 1.
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Synonym: 1-(5-Chloronaphthalene-1-sulfonyl)-1H-hexahydro-1,4-diazepine HCl;1-[(5-chloro-1-naphthalenyl)sulfonyl]hexahydro-1H-1,4-diazepine, monohydrochloride
Application: A selective inhibitor of MYLK, CaMK, PKB Kinase, PKA, and Stim1
CAS Number: 105637-50-1
Purity: ≥98%
Molecular Weight: 361.29
Molecular Formula: C15H17N2O2SCl•HCl
* Refer to Certificate of Analysis for lot specific data (including water content).
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ML-9 is a selective inhibitor of MYLK and CaMK that acts by delaying MYLK phosphorylation through binding at or near the ATP binding site. This naphthalenesulfonamide derivative has been shown to inhibit insulin-stimulated 2-deoxyglucose transport (IC50 = 27 μM), PP-1 activation in adipocytes, PKA, Akt1 (PKB) and Rsk (S6 kinase). ML-9 was also observed to disrupt microfilament bundles with accompanying decrease in P32 incorporation in rat astrocytes. Carbachol (sc-202092) illicited cationic currents were inhibitied with ML-9 (IC50 = 7.8 μM) in HEK293 cells. ML-9 has also demonstrated to inhibit natural killer cell lytic acitivity by regulating microfilament contraction as well as catecholamine secretion in intact and permeabilized chromaffin cells. In addition, agonist-induced Ca2+ entry into endothelial cells was completely abolished in the presence of ML-9. Shown to act as an inhibitor of Stim1, PKC and ERK.


References

1. Saitoh, M., et al. 1986. Biochem. Biophys. Res. Commun. 140: 280-287. PMID: 3778449
2. Saitoh, M., et al. 1987. J. Biol. Chem. 262: 7796-7801. PMID: 3108259
3. Ito, M., et al. 1989. Int. J. Immunopharmacol. 11: 185-190. PMID: 2703279
4. Inoue, G., et al. 1993. J. Biol. Chem. 268: 5272-5278. PMID: 7680348
5. Reig, J.A., et al. 1993. Neurochem. Res. 18: 317-323. PMID: 8479600
6. Begum, N., 1995. J. Biol. Chem. 270: 709-714. PMID: 7822300
7. Takahashi, R., et al. 1997. Biochem. Biophys. Res. Commun. 235: 657-662. PMID: 9207215
8. Smith, U., et al. 2000. Biochem. Biophys. Res. Commun. 268: 315-320. PMID: 10679201
9. Shi, J., et al. 2007. Br. J. Pharmacol. 152: 122-131. PMID: 17603544

Physical State :
Solid
Solubility :
Soluble in DMSO (10 mg/ml), ethanol:water 1:1 (10 mg/ml), DMSO:PBS (pH 7.2) 1:1 (~0.5 mg/ml), DMF (~30 mg/ml), water, and methanol.
Storage :
Store at -20° C
Melting Point :
191° C
Boiling Point :
508.8° C
IC50 :
PKB: IC50 = 10-50 µM; PKA: IC50 = 20 µM; S6 kinase: IC50 = 50 µM; MAP kinase: IC50 = ~35 µM
Ki Data :
MLC kinase: Ki= 3.8 µM; protein kinase A: Ki= 32 µM; protein kinase C: Ki= 54 µM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
108047
MDL Number :
MFCD00065525
SMILES :
C1CNCCN(C1)S(=O)(=O)C2=CC=CC3=C2C=CC=C3Cl.Cl

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Certificate of Analysis

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ML-9  Product Citations

See how others have used ML-9. Click on the entry to view the PubMed entry .

Citations 1 to 1 of 1 total

PMID: # 26213900  Bartolák-Suki, E. et al. 2015. Nat Mater. 14: 1049-57.

Citations 1 to 1 of 1 total

How long would you recommend storing aqueous solution?

Asked by: chemicalsmg
Thank you for your question. We do not recommend storing the aqueous solution for more than one day. Please contact Technical Service if you have further questions concerning this product.
Answered by: Tech Service 9
Date published: 2017-01-12

What is the solubility of this product?

Asked by: hawkeye11
Thank you for your question. The solubility of ML-9, sc-200519, is approximately 0.5 mg/ml in ethanol and approximately 30 mg/ml in DMSO and DMF
Answered by: TechService7
Date published: 2016-12-21
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Rated 5 out of 5 by from McCrudden CM; et al McCrudden CM; et al. (PubMed ID:25689628) utilized ML-9 as a positive control to inhibit myosin light chain kinase in rat arterial tissue. -SCBT Publication Review
Date published: 2015-06-13
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