Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T2033 |
BML-277
C 3742,Chk2 Inhibitor II,BML 277 |
Apoptosis; Chk | Apoptosis; Cell Cycle/Checkpoint |
BML-277 (C 3742) 是一种选择性的检测点激酶 2 抑制剂,IC50为 15 nM。 | |||
T6028 |
PF 477736
PF 00477736,PF-477736,PF-736,PF-00477736,PF477736 |
c-Fms; VEGFR; FGFR; FLT; c-RET; Chk; CDK; Src; Aurora Kinase | Angiogenesis; Apoptosis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Tyrosine Kinase/Adaptors |
PF 477736 (PF-736,PF-00477736) 是一种特异性、有效且具有 ATP 竞争性的 Chk1 抑制剂,Ki 值为0.49 nM。它也是Chk2抑制剂,Ki 值为 47 nM。它还抑制VEGFR2、Fms、Yes、Aurora-A、FGFR3、Flt3和Ret。 | |||
T10718L |
CCT241533 hydrochloride
|
Chk | Cell Cycle/Checkpoint |
CCT241533 hydrochloride is an effective and selective ATP competitive inhibitor of CHK2 (Ki: 1.16 nM; IC50: 3 nM). | |||
T13148 |
CHK-IN-1
|
Chk | Cell Cycle/Checkpoint |
CHK-IN-1 是一种具有抗增殖活性的 CHK1 和 CHK2 双重抑制剂。 | |||
T71259 |
GNE-900
GNE900,GNE 900 |
Apoptosis; Chk | Apoptosis; Cell Cycle/Checkpoint |
GNE-900 是一种 ATP 竞争性、选择性和口服活性 ChK1抑制剂,对 ChKl,ChK2的 IC50值分别为为 0.0011,1.5 µM。GNE-900 废除 G2-M 检查点,增强 DNA 损伤,并诱导胞凋亡 (Apoptosis)。gemcitabine 和 GNE-900 给药显示抗肿瘤活性[1]< /sup>。 | |||
T4327 |
Prexasertib dihydrochloride
LY2606368 (dihydrochloride),Prexasertib HCl,LY2606368 |
Apoptosis; Chk; S6 Kinase | Apoptosis; Cell Cycle/Checkpoint; MAPK; PI3K/Akt/mTOR signaling |
Prexasertib dihydrochloride (LY2606368) 是一种选择性的,ATP 竞争性的细胞周期检测点激酶 1 抑制剂,Ki 为 0.9 nM,IC50为 <1 nM。它抑制 CHK2(IC50=8 nM) 和 RSK1 (IC50=9 nM)。它引起双链 DNA 断裂和复制突变,导致细胞凋亡,有抗肿瘤活性。 | |||
T3700 |
SCH900776 (S-isomer)
MK-8776 S-isomer,SCH900776 S-isomer |
Chk; CDK | Cell Cycle/Checkpoint |
SCH900776 S-isomer (MK-8776 S-isomer) 是SCH900776的S 型同分异构体。 | |||
T6350 |
CHIR-124
CHIR124,CHIR 124 |
Apoptosis; GSK-3; FLT; Chk; PDGFR; Src | Angiogenesis; Apoptosis; Cell Cycle/Checkpoint; PI3K/Akt/mTOR signaling; Stem Cells; Tyrosine Kinase/Adaptors |
CHIR-124 是一种选择性 Chk1抑制剂,IC50值为 0.3 nM,可有效抑制 PDGFR 和 FLT3,IC50值分别为 6.6 nM 和 5.8 nM。 | |||
T15943 |
M443
|
p38 MAPK; Chk | Cell Cycle/Checkpoint; MAPK |
M443 是一种高效的 MRK 小分子抑制剂,抑制辐射诱导的 p38 和 Chk2 的激活,可用于研究癌症。 | |||
T7080 |
CCT245737
SRA737 |
Chk | Cell Cycle/Checkpoint |
CCT245737 (SRA737) 是一种具有口服活性的选择性 Chk1 抑制剂,IC50值为 1.3 nM。 | |||
T6093 |
AZD-7762
AZD7762 |
Chk | Cell Cycle/Checkpoint |
AZD-7762 是一种有效的 ATP 竞争性的细胞周期检测点激酶抑制剂,抑制 Chk1的 IC50为 5 nM。 | |||
T6940 |
PHA-767491 hydrochloride
CAY10572,PHA-767491,PHA767491 HCl,CAY-10572 hydrochloride |
Apoptosis; GSK-3; CDK | Apoptosis; Cell Cycle/Checkpoint; PI3K/Akt/mTOR signaling; Stem Cells |
PHA-767491 hydrochloride (CAY-10572 hydrochloride) 是一种Cdc7-Dbf4(DDK)/Cdk9的双重抑制剂,IC50值分别为 10 nM 和 34 nM。 | |||
T21331 |
SAR-020106
|
Chk | Cell Cycle/Checkpoint |
SAR-020106 是一种强效、ATP 竞争性和选择性 CHK1 抑制剂,IC50为 13.3 nM。它对 CHK2 具有良好的选择性,可通过选择抗癌药物增强抗肿瘤活性。 | |||
T2517 |
SCH900776
MK 8776,MK-8776 |
Chk; CDK | Cell Cycle/Checkpoint |
SCH900776 (MK-8776) 是一种靶向细胞周期检查点激酶 1(Chk1) 的抑制剂,IC50值为 3 nM。它比对 CDK2 和 Chk2 的选择性分别高 50 和 500 倍,具有潜在的放射增敏和化学增敏活性。 | |||
T10718 |
CCT241533
|
Chk | Cell Cycle/Checkpoint |
CCT241533 is an effective and selective ATP competitive inhibitor of CHK2 (Ki: 1.16 nM; IC50: 3 nM). | |||
T36704 |
CCT241533 dihydrochloride
CCT 241533 dihydrochloride |
||
Potent Chk2 inhibitor (IC50 = 3 nM). Shows >63-fold selectivity for Chk1 over Chk2 and a panel of 84 other kinases. Inhibits Chk2 activation in response to etoposide-induced DNA damage in HT29 cells. Blocks ionizing radiation-induced apoptosis of mouse thymocytes. Caldwell et al (2011) Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2. J.Med.Chem. 54 580 PMID:21186793 | |||
T17223 |
VER-00158411
|
Chk | Cell Cycle/Checkpoint |
VER-00158411 is a checkpoint kinase 1 and CHK2 inhibitor (IC50: 4.4 nM and 4.5 nM, respectively). | |||
T4310 |
Prexasertib
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 |
Apoptosis; Chk | Apoptosis; Cell Cycle/Checkpoint |
Prexasertib (LY2606368) 是一种具有潜在抗肿瘤活性的检查点激酶 1 抑制剂。它可引起双链 DNA 断裂和复制突变,导致细胞凋亡。 | |||
T23089 |
NSC 109555 ditosylate
|
Others | Others |
Chk2 inhibitor,ATP-competitive | |||
T29116 |
VRX-0466617
|
||
VRX-0466617 is a novel selective Chk2 inhibitor. | |||
T73411 |
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。PV-1019 抑制Topotecan 诱导的Chk2自磷酸化。PV-1019 抑制 IR 诱导的细胞凋亡。 | |||
T4310L |
Prexasertib lactate hydrate
Prexasertib monolactate monohydrate,LY-2606368,LY 2606368,LY2606368,Prexasertib monolactate monohydrate salt |
||
Prexasertib is an effective and selective Chk1/Chk2 inhibitor. Prexasertib causes Replication Catastrophe and Antitumor Effects through CHK1-Dependent Mechanisms. | |||
T4310L2 |
Prexasertib mesylate
LY-2606368,LY2606368,LY 2606368 |
||
Prexasertib is a potent and selective Chk1/Chk2 inhibitor. Prexasertib increases the effectiveness of conventional therapy in B-/T- cell progenitor acute lymphoblastic leukemia. LY2606368 causes replication catastrophe and antitumor effects through CHK1-d | |||
T24688 |
PV-1115
PV1115 |
||
PV-1115 is an effective and highly selective inhibitor of the Chk2. | |||
T38620 |
Prexasertib dimesylate
LY2606368 dimesylate |
||
Prexasertib dimesylate (LY2606368 dimesylate) is a highly selective ATP-competitive second-generation inhibitor of checkpoint kinase 1 (CHK1). With a K i of 0.9 nM and an IC 50 of <1 nM, Prexasertib dimesylate effectively inhibits CHK2 (IC 50 = 8 nM) and RSK1 (IC 50 = 9 nM). Its mechanism of action involves inducing double-stranded DNA breakage and replication catastrophe, ultimately leading to apoptosis. Moreover, Prexasertib dimesylate demonstrates potent anti-tumor activity. | |||
T71156 |
Poloxipan
|
||
Poloxipan is a potent and pan-specific PLK1 inhibitor. In vitro, Poloxipan has IC50 3.2 uM (Plk1); 1.7 uM (Plk2); and 3 uM (Plk3). Poloxipan showed minor inhibition over FHA dommain of Chk2, S2 domian of STAT1, STAT5b, Lck, etc. | |||
T33737 |
NSC 109555
NSC-109555,DDUG dimethanesulfonate,NSC109555,DDUG diMS |
||
NSC 109555 是一种选择性、可逆、ATP竞争性的Chk2抑制剂(IC50=0.2μM),对包括Chk1在内的一系列其他激酶没有影响(IC50>10μM)。抑制组蛋白H1磷酸化(IC50=0.24μM)并减弱线粒体ATP合成。在许多体内白血病中表现出抗增殖活性。 | |||
T63152 |
Prexasertib Mesylate Hydrate
|
||
Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) 是一种 ATP 竞争性的、选择性的第二代细胞周期检测点激酶 1 (CHK1) 抑制剂 (IC50<1 nM, Ki: 0.9 nM)。Prexasertib Mesylate Hydrate 对 CHK2 (IC50: 8 nM) 和 RSK1 (IC50: 9 nM) 表现出抑制作用。Prexasertib Mesylate Hydrate 能够导致双链 DNA 断裂和复制突变,诱导细胞凋亡,并表现出有效的抗肿瘤作用。 |