CKI-7

Modify Date: 2024-01-08 13:27:16

CKI-7 Structure
CKI-7 structure
Common Name CKI-7
CAS Number 120615-25-0 Molecular Weight 285.75000
Density 1.432g/cm3 Boiling Point 499.7ºC at 760mmHg
Molecular Formula C11H12ClN3O2S Melting Point 188-190ºC
MSDS N/A Flash Point 256ºC

 Use of CKI-7


CKI-7 is a potent and ATP-competitive casein kinase 1 (CK1) inhibitor with an IC50 of 6 μM and a Ki of 8.5 μM. CKI-7 is a selective Cdc7 kinase inhibitor. CKI-7 also inhibits SGK, ribosomal S6 kinase-1 (S6K1) and mitogen- and stress-activated protein kinase-1 (MSK1). CKI-7 has a much weaker effect on casein kinase II and other protein kinases[1][2][3][4].

 Names

Name N-(2-aminoethyl)-5-chloroisoquinoline-8-sulfonamide
Synonym More Synonyms

 CKI-7 Biological Activity

Description CKI-7 is a potent and ATP-competitive casein kinase 1 (CK1) inhibitor with an IC50 of 6 μM and a Ki of 8.5 μM. CKI-7 is a selective Cdc7 kinase inhibitor. CKI-7 also inhibits SGK, ribosomal S6 kinase-1 (S6K1) and mitogen- and stress-activated protein kinase-1 (MSK1). CKI-7 has a much weaker effect on casein kinase II and other protein kinases[1][2][3][4].
Related Catalog
Target

CK1:6 μM (IC50)

CK1:8.5 μM (Ki)

Cdc7

SGK

S6K1

MSK1

In Vitro CKI-7 (0.1-10 μM; 5 days; ES cells) treatment significantly increases the expression of the early neuroectodermal marker Sox1 and the number of cells positive for the neural markers nestin and βIII-tubulin, in a concentration-dependent manner[1]. CKI-7 (5 μM; 5 days; ES cells) treatment suppresses SFEB-induced β-catenin stabilization on day 5, indicating that CKI-7 inhibits Wnt signaling[1]. RT-PCR[1] Cell Line: Mouse ES cells Concentration: 0.1-10 μM Incubation Time: 5 days Result: Significantly increased the expression of the early neuroectodermal marker Sox1 and the number of cells positive for the neural markers nestin and βIII-tubulin, in a concentration-dependent manner. Western Blot Analysis[1] Cell Line: Mouse ES cells Concentration: 5 μM Incubation Time: 5 days Result: Suppressed SFEB-induced β-catenin stabilization on day 5.
In Vivo In vivo dose-dependent anti-tumor activity of CKI-7 is demonstrated in a SCID-Beige mouse systemic tumor model utilzing a recently isolated Philadelphia chromosome positive acute lymphoblastic leukemia cell line. Standard cell cycle synchronization studies established that exposure to CKI-7 results in cell cycle dependent caspase 3 activation and apoptotic cell death[2].
References

[1]. Osakada F, et al. In vitro differentiation of retinal cells from human pluripotent stem cells by small-molecule induction. J Cell Sci. 2009 Sep 1;122(Pt 17):3169-79.

[2]. Mark G. Frattini, et al. Small Molecule Inhibition of Cdc7, a Key Cell Cycle Regulator and Novel Therapeutic Target, Successfully Inhibits Leukemia Cell Growth in Vitro and in Vivo. Blood (2008) 112 (11): 2668.

[3]. Chijiwa T, et al. A newly synthesized selective casein kinase I inhibitor, N-(2-aminoethyl)-5-chloroisoquinoline-8-sulfonamide, and affinity purification of casein kinase I from bovine testis. J Biol Chem. 1989 Mar 25;264(9):4924-7.

[4]. Rena G, et al. D4476, a cell-permeant inhibitor of CK1, suppresses the site-specific phosphorylation and nuclear exclusion of FOXO1a. EMBO Rep. 2004 Jan;5(1):60-5.

 Chemical & Physical Properties

Density 1.432g/cm3
Boiling Point 499.7ºC at 760mmHg
Melting Point 188-190ºC
Molecular Formula C11H12ClN3O2S
Molecular Weight 285.75000
Flash Point 256ºC
Exact Mass 285.03400
PSA 93.46000
LogP 3.29720
Vapour Pressure 4.04E-10mmHg at 25°C
Index of Refraction 1.644

 Safety Information

Hazard Codes Xi
Risk Phrases R25
Safety Phrases S45
RIDADR UN 2811 6.1/PG 3
HS Code 2935009090

 Customs

HS Code 2935009090
Summary 2935009090 other sulphonamides VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:35.0%

 Synonyms

N-(2-Aminoethyl)-5-chloroisoquinoline-8-sulphonamide
CKI-7
2csn
CKI
8-Isoquinolinesulfonamide,N-(2-aminoethyl)-5-chloro