CLK
he CDC-like protein kinases are a widespread family of splice factor kinases involved in normal physiology and in several diseases including cancer. In humans they include the CLK1, CLK2, CLK3 and CLK4 genes. The expression of CLK1 is regulated through alternative splicing producing both full-length catalytically active and truncated catalytically inactive isoforms, CLKT1 (arising from exon 4 skipping) and CLKT2 (arising from intron 4 retention). CLK kinases phosphorylate the so-called ‘SR protein’ splice factors, facilitating their activation and release from nuclear speckles. CLK kinases can also phosphorylate non-SR protein splice factors including the spliceosome-associated SPF45. CLK activity is increasingly associated with the development and progression of cancer. As a result there is considerable interest in developing selective CLK inhibitors that block tumour growth. CLK1 is also a potential target in the treatment of Alzheimer's and has been earmarked for the treatment of Duchenne's muscular dystrophy as its inhibition causes the skipping of a mutated exon. CLK targeting has also been proposed for the treatment of viral infection including HIV-1 and influenza.
References
1.Dale P Corkery,et al. Nucleus. 2015; 6(4): 279–288.
References
1.Dale P Corkery,et al. Nucleus. 2015; 6(4): 279–288.
Cell Cycle/DNA Damage
ABC(12)
AChR(104)
Antifolate(12)
ATM/ATR(26)
Aurora Kinase(51)
CLK(15)
c-Myc(22)
DHFR(16)
DNA Alkylator(34)
DNA gyrase(11)
DNA Repair Protein(21)
DNA/RNA Synthesis(187)
DNA-PK(15)
GPR(97)
HDAC(152)
Hec1/Nek2(9)
Integrin(77)
LIM Kinase (LIMK)(7)
Mps1/TTK(2)
Nucleoside Antimetabolite/Analog(48)
Other Targets(4)
PAK(13)
PARP(67)
PLK(26)
Potassium Channel(146)
RAD51(1)
Rho(16)
ROCK(42)
Telomerase(12)
Topoisomerase(88)
Wee1(7)
CLK
-
KuWal151
产品货号 : M16943
cas no: ——
KuWal151 是一种有效的选择性 cdc2 样激酶 (CLK) 抑制剂,对 CLK1/2/4 的 IC50 分别为 88/510/28 nM。 -
T-025
产品货号 : M16935
cas no: ——
T-025(T025,CLK 抑制剂 T-025)是一种口服有效的 Cdc2 样激酶 (CLK) 抑制剂,对于 CLK1、CLK2、CLK3 和 CLK4 的 Kd 分别为 4.8、0.096、6.5 和 0.61 nM。抑制 DYRK1A 和 DYRK1B,IC50 分别为 0.074 和 1.5 nM。 -
CLK2 inhibitor Indazole1
产品货号 : M16934
cas no: ——
CLK2 抑制剂 Indzo1 是一种新型有效的选择性 CLK2 抑制剂,IC50 为 2.7 nM。 -
TG693
产品货号 : M16408
cas no: 885272-55-9
TG693 是一种口服、选择性、ATP 竞争性 CLK1 抑制剂,IC50 为 112.6 nM。 -
K00546
产品货号 : M14518
cas no: 443798-47-8
K00546 是 CDC2 样激酶 CLK1 和 CLK3 的有效抑制剂,IC50 分别为 8.9 和 29.2 nM。