PKCμ

PKCµ, now designated PKD1, is a diacylglycerol- and phorbol ester-responsive serine/threonine kinase with a distinctive catalytic domain^[1]. Mechanistically, PKCµ/PKD1 regulates transport-carrier fission from the trans-Golgi network and links membrane trafficking to cell-surface delivery^[2]. This trafficking role connects directly with cell adhesion because PKD1/PKCµ promotes αvβ3 integrin recycling and delivery to nascent focal adhesions^[3]. In gastric cancer models, PKD1 promoter methylation correlated with reduced PKD1 expression, and PKD1 downregulation affected migration and invasiveness^[4]. Compared with related isoforms, PKD1 and PKD2 show non-redundant functions in vivo, with PKD1 catalytic activity required for normal embryogenesis whereas PKD2 catalytic activity was dispensable for that process^[5]. For experimental applications, PKD inhibitors provide tools to test PKD-dependent proliferation, migration, survival, and pathway activation in cancer models^[6]^[7].

References:

[1]. Valverde AM, et al. Molecular cloning and characterization of protein kinase D: a target for diacylglycerol and phorbol esters with a distinctive catalytic domain. Proc Natl Acad Sci U S A. 1994 Aug 30;91(18):8572-6. [Content Brief]

[2]. Liljedahl M, et al. Protein kinase D regulates the fission of cell surface destined transport carriers from the trans-Golgi network. Cell. 2001 Feb 9;104(3):409-20. [Content Brief]

[3]. Woods AJ, et al. PKD1/PKCmu promotes alphavbeta3 integrin recycling and delivery to nascent focal adhesions. EMBO J. 2004 Jul 7;23(13):2531-43. [Content Brief]

[4]. Kim M, et al. Epigenetic inactivation of protein kinase D1 in gastric cancer and its role in gastric cancer cell migration and invasion. Carcinogenesis. 2008 Mar;29(3):629-37. [Content Brief]

[5]. Matthews SA, et al. Unique functions for protein kinase D1 and protein kinase D2 in mammalian cells. Biochem J. 2010 Nov 15;432(1):153-63. [Content Brief]

[6]. Ali SR, et al. Nerve Density and Neuronal Biomarkers in Cancer. Cancers (Basel). 2022 Oct 1;14(19):4817. [Content Brief]

[7]. Meredith EL, et al. Identification of potent and selective amidobipyridyl inhibitors of protein kinase D. J Med Chem. 2010 Aug 12;53(15):5422-38. [Content Brief]

PKCμ Inhibitors (2)

PKCμ 관련 제품 (2):

By Type:	Pan (2)

Cat. No.	상품명	효과	Purity

HY-13689

Go 6983	Inhibitor	99.23%
Go 6983 is a pan-PKC inhibitor against for PKCα, PKCβ, PKCγ, PKCδ and PKCζ with IC₅₀ of 7 nM, 7 nM, 6 nM, 10 nM and 60 nM, respectively.

HY-16903

MS-553	Inhibitor	99.79%
MS-553 is a potent, ATP-competitive and reversible inhibitor of conventional PKC enzymes with K_is of 5.3 and 10.4 nM for human PKCβ and PKCα, and IC₅₀s of 2.3, 8.1, 7.6, 25.6, 57.5, 314, 808 nM for PKCα, PKCβI, PKCβII, PKCθ, PKCγ, PKC mu and PKCε, respectively.

Name
이메일 *

	Sorry, but the email address you supplied was invalid.