Checkpoint Kinase (Chk)(细胞周期检查点激酶)
Checkpoint Kinases (Chk) are protein kinases that are involved in cell cycle control. Two checkpoint kinase subtypes have been identified, Chk1 and Chk2. Chk1 is a central component of genome surveillance pathways and is a key regulator of the cell cycle and cell survival. Chk1 is required for the initiation of DNA damage checkpoints and has recently been shown to play a role in the normal (unperturbed) cell cycle. Chk1 impacts various stages of the cell cycle including the S phase, G2/M transition and M phase. In addition to mediating cell cycle checkpoints, Chk1 also contributes to DNA repair processes, gene transcription, embryo development, cellular responses to HIV infection and somatic cell viability. Chk2 is a protein kinase that is activated in response to DNA damage and is involved in cell cycle arrest. In response to DNA damage and replication blocks, cell cycle progression is halted through the control of cell cycle regulators. The protein encoded by this gene is a cell cycle checkpoint regulator and putative tumor suppressor.
Products for Checkpoint Kinase (Chk)
- Cat.No. 产品名称 Information
- GC73822 GNE-900 GNE-900是一种ATP竞争性、选择性和口服活性的ChK1抑制剂,ChKl和ChK2的IC50分别为0.0011和1.5µM。
- GC72986 CHK1-IN-4 hydrochloride CHK1-IN-4 hydrochloride(化合物3)是一种强效的检查点激酶1(chk1)抑制剂,能有效抑制肿瘤细胞中的chk1磷酸化。
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GC72958
PV-1019
NSC 744039
PV-1019(NSC 744039)是一种有效的选择性Chk2抑制剂,IC50值为24 nM。 - GC72784 VRX0466617 VRX0466617一种选择性Chk2抑制剂,抑制Chk2-Ser 19和Ser33-35的磷酸化。
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GC65435
Monalizumab
莫那利珠单抗
Monalizumab 是一种首创的靶向自然杀伤细胞群 2A (NKG2A) 的免疫检查点抑制剂。Monalizumab 是一种人源化抗 NKG2A 的单克隆抗体,可增加 IFN-γ 产生,从而促进自然杀伤细胞功能。Monalizumab 可用于头颈部鳞状细胞癌 (HNSCC) 的研究。
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GC62986
GDC-0425
5-((1-乙基哌啶-4-基)氧基)-9H-吡咯并[2,3-B:5,4-C']二吡啶-6-甲腈,RG-7602
GDC-0425 (RG-7602) 是一种有效的、具有口服活性的、高选择性的 ChK1 抑制剂。GDC-0425 可用于多种恶性肿瘤的研究。 - GC49430 Wee1 Inhibitor An inhibitor of Wee1
- GC60698 Chk1-IN-5 Chk1-IN-5是有效的检查点激酶1(Chk1)抑制剂。Chk1-IN-5抑制Chk1磷酸化,并在结肠癌异种移植模型中抑制肿瘤生长。
- GC50119 AZD 7762 hydrochloride A selective checkpoint kinase inhibitor
- GC50085 CCT 241533 dihydrochloride CCT 241533 dihydrochloride 是一种有效的选择性 ATP 竞争性 CHK2 抑制剂,IC50 为 3 nM,Ki 为 1.16 nM。
- GC39284 ANI-7 ANI-7 是一种 AhR 途径的激活剂。ANI-7 抑制多种癌细胞的生长,并有选择地抑制 MCF-7 乳腺癌细胞的生长,GI50 为 0.56 μM。ANI-7 通过激活 AhR 途径诱导 CYP1 代谢单加氧酶,并在敏感的乳腺癌细胞系中诱导 DNA 损伤,检查点激酶 (Chk2) 激活,S 期细胞周期停滞和细胞死亡。
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GC36967
Prexasertib Mesylate Hydrate
LY2606368 Mesylate Hydrate; LY2940930
Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) 是一种有效、选择性、 ATP 竞争性的 CHK1 和 CHK2 抑制剂,对 CHK1 的 Ki 值为 0.9 nM,IC50 值 <1 nM,对 CHK2 的 IC50 值为 8 nM。Prexasertib Mesylate Hydrate 抑制 HT-29 细胞 CHK1 (S296) 和 CHK2 (S516) 的自身磷酸化。Prexasertib Mesylate Hydrate 具有高效抗肿瘤活性,在 HeLa 细胞中,消除 G2/M 检查点,EC50 值为 9 nM。 -
GC36966
Prexasertib dihydrochloride
CHK1抑制剂,LY2606368 dihydrochloride
Prexasertib (LY2606368) is an ATP-competitive CHK1 inhibitor with a Ki value of 0.9 nmol/L. For CHK2 and RSK, its IC50 values are 8 nM and 9 nM respectively in cell-free assay. - GC35679 CHK1-IN-3 CHK1-IN-3 是一种检测点激酶 (CHK1) 抑制剂,IC50 值为 0.4 nM。
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GC34127
GDC-0575 dihydrochloride (ARRY-575 dihydrochloride)
ARRY-575 dihydrochloride; RG7741 dihydrochloride
A Chk1 inhibitor - GC33392 CHK-IN-1 CHK-IN-1是一种CHK1和CHK2的抑制剂,具有抗增殖作用。
- GC33289 CHK1-IN-2 CHK1-IN-2是细胞周期检测点激酶(CHK1)的抑制剂,其IC50为6nM。
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GC32885
GDC-0575 (ARRY-575, RG7741)
(R)-N-(4-(3-氨基哌啶-1-基)-5-溴-1H-吡咯并[2,3-B]吡啶-3-基)环丙烷甲酰胺,ARRY-575; RG7741
A Chk1 inhibitor -
GC30106
CHK1 inhibitor
GDC-0575 analog
CHK1inhibitor是CHK1的抑制剂。 - GC19093 CCT245737 A potent Chk1 inhibitor
- GC18396 PD 407824 An inhibitor of Chk1 and WEE1
- GC11022 SB 218078 A potent Chk1 inhibitor
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GC14772
CCT244747
3-[(1R)-2-(二甲基氨基)-1-甲基乙氧基]-5-[[4-甲氧基-5-(1-甲基-1H-吡唑-4-基)-2-吡啶基]氨基]-2-吡嗪甲腈
A potent Chk1 inhibitor -
GC15663
LY2606368
5-[[5-[2-(3-氨基丙氧基)-6-甲氧基苯基]-1H-吡唑-3-基]氨基]-2-吡嗪甲腈,LY2606368
LY2606368 是一种 ATP 竞争性 CHK1 抑制剂,目前处于临床阶段,Ki 为 0.9 nM,IC50 <1 nM。 -
GC11648
BML-277
Chk2 Inhibitor II
A selective DNA damage control kinase inhibitor -
GC14234
PF-477736
PF 00477736
A selective inhibitor of checkpoint kinase 1 -
GC15741
LY2603618
LY2603618; IC-83
A Chk1 inhibitor -
GC15739
CHIR-124
4-[((3S)-1-氮杂双环[2,2,2]辛-3-基)氨基]-3-(1H-苯并咪唑-2-基)-6-氯喹啉-2(1H)-酮
A selective Chk1 inhibitor -
GC16374
MK-8776(SCH-900776)
6-溴-3-(1-甲基-1H-吡唑-4-基)-5-(3R)-3-哌啶基吡唑并[1,5-A]嘧啶-7-胺,MK-8776
A selective Chk1 inhibitor -
GC10546
AZD7762
3-[(氨基羰基)氨基]-5-(3-氟苯基)-N-(3S)-3-哌啶基-2-噻吩羧胺
A selective checkpoint kinase inhibitor -
GC17105
CCT241533 hydrochloride
CCT241533盐酸盐,CCT-241533 hydrochloride;CCT 241533 hydrochloride
A selective Chk2 inhibitor -
GC18053
CCT241533
(3R,4S)-4-[[2-(5-氟-2-羟基苯基)-6,7-二甲氧基-4-喹唑啉基]氨基]-ALPHA,ALPHA-二甲基-3-吡咯烷甲醇,CCT 241533;CCT-241533
A selective Chk2 inhibitor