KN-93An effective inhibitor of CaMKII phosphorylating activity

KN-93 (CAS 139298-40-1)

KN-93 | CAS 139298-40-1 is rated 5.0 out of 5 by 1.
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Synonym: N-[2-[[[(E)-3-(4-chlorophenyl)prop-2-enyl]-methylamino]methyl]phenyl]-N-(2-hydroxyethyl)-4-methoxybenzenesulfonamide
Application: An effective inhibitor of CaMKII phosphorylating activity
CAS Number: 139298-40-1
Purity: ≥95%
Molecular Weight: 501.04
Molecular Formula: C26H29ClN2O4S
* Refer to Certificate of Analysis for lot specific data (including water content).
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KN-93 is a methoxybenzenesulfonamide that is an effective inhibitor of CaMKII (Ca2+/calmodulin-dependent protein kinase II) phosphorylating activity, and the autophosphorylation of the α- and β-subunits of CaMKII. In PC-12h cells, KN-93 has been shown to decrease phosphorylation of KCl and acetylcholine. Data suggests that KN-93 modulates the reaction rate of TH by reducing the Ca2+ mediated phosphorylation levels of TH and inhibiting dopamine formation. In rat pancreatic beta cell studies, KN-93 was shown to block insulin release, and in prostrate cancer research, KN-93 inhibited androgen receptor function and enhanced cell death independent of p53 and Akt. Research indicates that KN-93 induces G1 cell cycle arrest in both HeLa (sc-2200) and NIH 3T3 fibroblast cells (sc-2210), and causes apoptosis in NIH 3T3 cells.


References

1. Sumi, M., et al. 1991. Biochem. Biophys. Res. Commun. 181: 968-975. PMID: 1662507
2. Niki, I., et al. 1993. Biochem. Biophys. Res. Commun. 191: 255-261. PMID: 8383489
3. Rasmussen, G., et al. 1995. Biochem. Cell Biol. 73: 201-207. PMID: 7576494
4. Tombes, R.M., et al. 1995. Cell Growth Differ. 6: 1063-1070. PMID: 8519682
5. Rokhlin, O.W., et al. 2010. Cancer Biol. Ther. 9: 224-235. PMID: 20023417

Usage :
• KN-93 should be dissolved in ethanol first and then diluted with the aqueous buffer of choice, for maximum solubility in aqueous buffers.

• Approximately 0.25 mg/ml of KN-93 can be solubilized in a 1:2 solution of ethanol:PBS (pH 7.2) using this method.

• it is not recommended to store aqueous solution more than one day.

• KN-93 is sparingly soluble in aqueous buffers.
Physical State :
Solid
Solubility :
Soluble in DMSO (25 mg/ml), water, 1:2 EtOH:PBS(pH 7.2) (~0.25 mg/ml), ethanol (~30 mg/ml), and DMF (~30 mg/ml).
Storage :
Store at -20° C
Boiling Point :
~657.60° C at 760 mmHg (Predicted)
Density :
~1.3 g/cm3 (Predicted)
Refractive Index :
n20D 1.63
IC50 :
CaM kinase II: IC50 = 370 nM; histamine-induced aminopyrine uptake: IC50 = 300 nM (parietal cells)
Ki Data :
CaM binding to the kinase II: Ki= 370 nM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
5312122
MDL Number :
MFCD00236424
SMILES :
CN(C/C=C/C1=CC=C(C=C1)Cl)CC2=CC=CC=C2N(CCO)S(=O)(=O)C3=CC=C(C=C3)OC

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Certificate of Analysis

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KN-93  Product Citations

See how others have used KN-93. Click on the entry to view the PubMed entry .

Citations 1 to 10 of 21 total

PMID: # 31396050  Kim, JE.|Kang, TC.| et al. 2019. Front Mol Neurosci. 12: 180.

PMID: # 29805077  Takahashi, N.|Chen, HY.|Harris, IS.|Stover, DG.|Selfors, LM.|Bronson, RT.|Deraedt, T.|Cichowski, K.|Welm, AL.|Mori, Y.|Mills, GB.|Brugge, JS.| et al. 2018. Cancer Cell. 33: 985-1003.e7.

PMID: # 28842328  Regazzetti, C. et al. 2017. The Journal of investigative dermatology.

PMID: # 29017032  Rajan, A.|Housden, BE.|Wirtz-Peitz, F.|Holderbaum, L.|Perrimon, N.| et al. 2017. Dev. Cell. 43: 83-98.e6.

PMID: # 28692053  Tsoi, H. et al. 2017. Oncogene. 36: 6109-6118.

PMID: # 27864646  Yan, X. et al. 2017. Lasers Med Sci. 32: 169-180.

PMID: # 28971270  Shi, D. et al. 2017. Inflammation.

PMID: # 28767177  Hinrichsen, I. et al. 2017. Mol. Carcinog. 56: 2663-2668.

PMID: # 27245989  Wang, Q. et al. 2016. Autophagy. 1-15.

PMID: # 27012864  Gu, Y. et al. 2016. Leukemia.

Citations 1 to 10 of 21 total

Should this product be protected from light?

Asked by: chemicalsmg
Thank you for your question. KN-93 (CAS 139298-40-1), should be protected from light during handling and storage.
Answered by: Chemical Support 3
Date published: 2018-08-20

What is the appearance of the compound?

Asked by: two2igm05
Thank you for your question. The compound, sc-202199, is provided as an off-white powder. If you have any further questions or concerns, please feel free to contact our Technical Service department by calling 800-457-3801 option 2, emailing scbt@scbt.com, or using the Live Chat function on our website.
Answered by: Tech Service 8
Date published: 2017-01-18
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Rated 5 out of 5 by from Flamand Flamand, et. al. (PubMed ID 18978352) found that KN-93, a Calcium/calmodulin dependent kinase II, can induce the nuclear export of 5-LO. NIH 3T3, HeLa and COS-1 cells were used. -SCBT Publication Review
Date published: 2015-06-25
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