KN-92 - CAS 176708-42-2
Catalog number: 176708-42-2
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C24H25ClN2O3S
Molecular Weight:
456.98
COA:
Inquire
Targets:
CaMK-II
Description:
KN-92 is intended to be used as a control compound in studies designed to elucidate the antagonist activities of KN-93. KN-93 inhibits histamine-induced aminopyrine uptake in parietal cells (IC50 = 300 nM). KN-93 has been used to implicate roles for CaMKII in Ca2+-induced Ca2+ release in cardiac myocytes, constitutive phosphorylation of 5-lipoxygenase in 3T3 cells, and Ca2+-dependent activation of HIF-1α in colon cancer cell.
Purity:
>98%
Synonyms:
KN 92; KN92
MSDS:
Inquire
InChIKey:
RUAOVVIUGUOYHA-AATRIKPKSA-N
InChI:
InChI=1S/C24H25ClN2O3S/c1-27(17-5-6-19-9-11-21(25)12-10-19)18-20-7-3-4-8-24(20)26-31(28,29)23-15-13-22(30-2)14-16-23/h3-16,26H,17-18H2,1-2H3/b6-5+
Canonical SMILES:
CN(CC=CC1=CC=C(C=C1)Cl)CC2=CC=CC=C2NS(=O)(=O)C3=CC=C(C=C3)OC
1.Role of calmodulin-calmodulin kinase II, cAMP/protein kinase A and ERK 1/2 on Aeromonas hydrophila-induced apoptosis of head kidney macrophages.
Banerjee C;Khatri P;Raman R;Bhatia H;Datta M;Mazumder S PLoS Pathog. 2014 Apr 24;10(4):e1004018. doi: 10.1371/journal.ppat.1004018. eCollection 2014 Apr.
The role of calcium (Ca2+) and its dependent protease calpain in Aeromonas hydrophila-induced head kidney macrophage (HKM) apoptosis has been reported. Here, we report the pro-apoptotic involvement of calmodulin (CaM) and calmodulin kinase II gamma (CaMKIIg) in the process. We observed significant increase in CaM levels in A. hydrophila-infected HKM and the inhibitory role of BAPTA/AM, EGTA, nifedipine and verapamil suggested CaM elevation to be Ca2+-dependent. Our studies with CaM-specific siRNA and the CaM inhibitor calmidazolium chloride demonstrated CaM to be pro-apoptotic that initiated the downstream expression of CaMKIIg. Using the CaMKIIg-targeted siRNA, specific inhibitor KN-93 and its inactive structural analogue KN-92 we report CaM-CaMKIIg signalling to be critical for apoptosis of A. hydrophila-infected HKM. Inhibitor studies further suggested the role of calpain-2 in CaMKIIg expression. CaMK Kinase (CaMKK), the other CaM dependent kinase exhibited no role in A. hydrophila-induced HKM apoptosis. We report increased production of intracellular cAMP in infected HKM and our results with KN-93 or KN-92 implicate the role of CaMKIIg in cAMP production. Using siRNA to PKACA, the catalytic subunit of PKA, anti-PKACA antibody and H-89, the specific inhibitor for PKA we prove the pro-apoptotic involvement of cAMP/PKA pathway in the pathogenicity of A.
2.Apoptosis induced by NAD depletion is inhibited by KN-93 in a CaMKII-independent manner.
Takeuchi M;Yamamoto T Exp Cell Res. 2015 Jul 1;335(1):62-7. doi: 10.1016/j.yexcr.2015.05.019. Epub 2015 May 27.
Nicotinamide phosphoribosyltransferase (NAMPT) is a key enzyme that catalyzes the synthesis of nicotinamide mononucleotide from nicotinamide (Nam) in the salvage pathway of mammalian NAD biosynthesis. Several potent NAMPT inhibitors have been identified and used to investigate the role of intracellular NAD and to develop therapeutics. NAD depletion induced by NAMPT inhibitors depolarizes mitochondrial membrane potential and causes apoptosis in a range of cell types. However, the mechanisms behind this depolarization have not been precisely elucidated. We observed that apoptosis of THP-1 cells in response to NAMPT inhibitors was reduced by the Ca(2+)/calmodulin-dependent protein kinase II (CaMKII) inhibitor KN-93 via an unknown mechanism. The inactive analog of KN-93, KN-92, exhibited the same activity, but the CaMKII-inhibiting cell-permeable autocamtide-2-related inhibitory peptide II did not, indicating that the inhibition of THP-1 cell apoptosis was not dependent on CaMKII. In evaluating the mechanism of action, we confirmed that KN-93 did not inhibit decreases in NAD levels but did inhibit decreases in mitochondrial membrane potential, indicating that KN-93 exerts inhibition upstream of the mitochondrial pathway of apoptosis.
3.The Ca++/calmodulin-dependent protein kinase II inhibitors KN62 and KN93, and their inactive analogues KN04 and KN92, inhibit nicotinic activation of tyrosine hydroxylase in bovine chromaffin cells.
Marley PD;Thomson KA Biochem Biophys Res Commun. 1996 Apr 5;221(1):15-8.
The possible role of Ca++/calmodulin-dependent protein kinase II (CAM-K-II) in the nicotinic activation of tyrosine hydroxylase in intact cultured bovine adrenal chromaffin cells has been investigated. Over the concentration range 3-30 microM, KN62, a specific CAM-K-II inhibitor, inhibited basal tyrosine hydroxylase activity and the activity stimulated by nicotine or K+ depolarisation. KN04, a structural analogue of KN62 which does not inhibit CAM-K-II, produced an identical concentration-dependent inhibition of basal and nicotine-stimulated tyrosine hydroxylase activity. Another CAM-K-II inhibitor, KN93, also inhibited nicotine and K+ stimulation of tyrosine hydroxylase activity; however, an inactive analogue of KN93, KN92, mimicked these effect. The results suggest that the inhibition of nicotine- and K+-stimulated tyrosine hydroxylase activity by KN62 and KN93 is not due to their ability to inhibit CAM-K-II.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related CaMK-II Products


CAS 201422-04-0 Autocamtide-2-related inhibitory peptide, myristoylated

Autocamtide-2-related inhibitory peptide
(CAS: 201422-04-0)

Autocamtide-2-related inhibitory peptide, myristoylated is a CaM kinase II inhibitor. It is an enhanced cell-permeable derivative of autocamtide-2-related inhib...

CAS 224579-74-2 MLCK inhibitor peptide 18

MLCK inhibitor peptide 18
(CAS: 224579-74-2)

A myosin light chain kinase (MLCK) inhibitor (IC50= 50 nM), and inhibits CaM kinase IIonly at 4000-fold higher concentrations.

CAS 52029-86-4 STO-609

STO-609
(CAS: 52029-86-4)

STO-609, a naphthoyl fused benzimidazole cell-permeable compound, is a potent and ATP-competitive inhibitor of the Ca2+/Calmodulin-dependent protein kinase kina...

CAS 118458-54-1 Arcyriaflavin A

Arcyriaflavin A
(CAS: 118458-54-1)

Arcyriaflavin A is a potent dual target agent of calcium/calmodulin-dependent protein kinase II (CaMKII) and cyclin-dependent kinase 4 (CDK4). Its IC50 values a...

CAS 108334-68-5 Syntide 2

Syntide 2
(CAS: 108334-68-5)

Syntide 2, a synthetic peptide, is recognized as a substrate by Ca2+/calmodulin-dependent protein kinase II (CaMKII) (Ki= 12 μM) and protein kinase C (Km = 11 µ...

CAS 139298-40-1 KN-93

KN-93
(CAS: 139298-40-1)

KN-93 is a selective Ca2+/calmodulin-dependent protein kinase II inhibitor, which has been implicated in the regulation of smooth muscle contractility. CaM kina...

CAS 1431698-47-3 KN-92 hydrochloride

KN-92 hydrochloride
(CAS: 1431698-47-3)

KN-92 is an inactive derivative of KN-93, the selective inhibitor of Ca2+/calmodulin-dependent kinase type II (CaMKII). At concentrations up to 25 μM, KN-92 is ...

CAS 176708-42-2 KN-92

KN-92
(CAS: 176708-42-2)

KN-92 is intended to be used as a control compound in studies designed to elucidate the antagonist activities of KN-93. KN-93 inhibits histamine-induced aminopy...

CAS 167114-91-2 Autocamtide-2-related inhibitory peptide

Autocamtide-2-related inhibitory peptide
(CAS: 167114-91-2)

Autocamtide-2-related inhibitory peptide is a highly selective, specific and potent inhibitor of calmodulin-dependent protein kinase II (CaM kinase II) with I50...

CAS 1188890-40-5 KN 93

KN 93
(CAS: 1188890-40-5)

KN 93 is an inhibitor of multifunctional Calmodulin-dependent protein kinase (CaMKII; Ki value 0.37 μM for inhibition of CaMKII phosphorylating activity). KN93 ...

CAS 1135280-28-2 KN-92 phosphate

KN-92 phosphate
(CAS: 1135280-28-2)

KN-92 is an inactive analog of the CaM kinase II inhibitor KN 93.

CAS 1208123-85-6 CaMKII-IN-1

CaMKII-IN-1
(CAS: 1208123-85-6)

CaMKII-IN-1 is a potent and highly selective CaMKII inhibitor with IC50 of 63 nM; significantly high selectivity against CaMKIV, MLCK, p38a, Akt1, and PKC.

Chemical Structure

CAS 176708-42-2 KN-92

Quick Inquiry

Verification code

Featured Items