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1177141-67-1

1177141-67-1 structure
1177141-67-1 structure
  • Name: CKI-7 HCl
  • Chemical Name: N-(2-Aminoethyl)-5-chloroisoquinoline-8-sulfonamide Dihydrochloride
  • CAS Number: 1177141-67-1
  • Molecular Formula: C11H14Cl3N3O2S
  • Molecular Weight: 358.67200
  • Catalog: Signaling Pathways Cell Cycle/DNA Damage Casein Kinase
  • Create Date: 2016-10-20 06:27:16
  • Modify Date: 2025-08-26 18:20:08
  • 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].

Name N-(2-Aminoethyl)-5-chloroisoquinoline-8-sulfonamide Dihydrochloride
Synonyms N-(2-Aminoethyl)-5-chloroisoquinoline-8-sulphonamide dihydrochloride
CKI-7 dihydrochloride
N-(2-Aminoethyl)-5-chloro-8-isoquinolinesulfonamide dihydrochlori de
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.

Molecular Formula C11H14Cl3N3O2S
Molecular Weight 358.67200
Exact Mass 356.98700
PSA 93.46000
LogP 4.90120
Storage condition -20°C
Symbol GHS06
GHS06
Signal Word Danger
Hazard Statements H301
Precautionary Statements P301 + P310
Personal Protective Equipment Eyeshields;Faceshields;Gloves;type P2 (EN 143) respirator cartridges
Hazard Codes T+
RIDADR UN 2811 6.1 / PGIII
Hazard Class 6.1
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