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Search Results for " chk1 "

Targets Recommended: Chk

58

抑制剂 & 化合物

1

天然产物

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重组蛋白

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Cat. No.	Product Name	Target	Signaling Pathways
T10792L	CHK1-IN-4 hydrochloride CHK1-IN-4 hydrochloride（2120398-41-4 Free base）	Chk	Cell Cycle/Checkpoint
	CHK1-IN-4 hydrochloride 是有效的checkpoint kinase 1 (chk1) 抑制剂，对肿瘤细胞中 chk1 磷酸化具有有效的抑制作用。CHK1-IN-4 hydrochloride 显示出抗肿瘤活性。
T10791	CHK1-IN-3	Chk	Cell Cycle/Checkpoint
	CHK1-IN-3 是一种检测点激酶 (CHK1) 抑制剂，IC50 值为 0.4 nM。
T37098	Chk1-IN-5 Chk1-IN-5
	Chk1-IN-5 is a highly effective inhibitor of checkpoint kinase 1 (Chk1), which hinders the phosphorylation of Chk1 and effectively suppresses tumor growth in a colon cancer xenograft model[1].
T40091	Chk1-IN-6 Chk1-IN-6
	Chk1-IN-6 is a potent, selective, and orally bioavailable CHK1 inhibitor candidate.
T10790	CHK1-IN-2	Chk	Cell Cycle/Checkpoint
	CHK1-IN-2 is an inhibitor of checkpoint kinase 1 (CHK1; IC50: 6 nM).
T10793	CHK1 inhibitor GDC-0575 analog	Chk	Cell Cycle/Checkpoint
	CHK1 inhibitor (GDC-0575 analog) is a CHK1 inhibitor.
T10792	CHK1-IN-4	Chk	Cell Cycle/Checkpoint
	CHK1-IN-4 is a potent inhibitor of checkpoint kinase 1 (chk1) and potently inhibits chk1 phosphorylation in the tumor cells with anti-tumor activity.
T82393	FLT3/CHK1-IN-1
	FLT3/CHK-IN-1（Compound 18）为FLT3/CHK1双重抑制剂，其对c-KIT的选择性超1700倍，同时显著降低对hERG的亲和力，IC50为58.4 μM。在MV-4-11细胞接种小鼠异种移植模型中有效抑制肿瘤生长。
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。
T6931	PD0166285 PD-166285	Apoptosis; Wee1; Chk	Apoptosis; Cell Cycle/Checkpoint
	PD0166285是 P-gp 的底物，是一种有效的 Wee1 和 Chk1 抑制剂弱抑制。
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。
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。
T27407	GDC0575 monohydrochloride ARRY-575,GDC-0575,GDC 0575,ARRY575,GDC0575	Chk	Cell Cycle/Checkpoint
	GDC0575 monohydrochloride (ARRY575) 是一种有效的、选择性的细胞周期检查点激酶 1(Chk1) 抑制剂，IC50 为 1.2 nM。GDC0575 monohydrochloride (ARRY575) 特异性结合并抑制 Chk1；这可能导致肿瘤细胞在 S 期和 G2/M 期绕过 Chk1 依赖性细胞周期停滞，从而允许细胞在进入有丝分裂之前进行 DNA 修复。
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。
T7300	GDC-0575 ARRY-575,RG7741	Chk	Cell Cycle/Checkpoint
	GDC-0575 (ARRY-575) 是一种高选择性，有口服活性的小分子Chk1抑制剂，IC50值为1.2 nM。
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。
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。
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。
T16446	PD 407824 PD-407824	Wee1; Chk	Cell Cycle/Checkpoint
	PD 407824 是一种化学 BMP 增敏剂，能促进细胞对亚阈值量 BMP4 的敏感性提高。PD 407824 是一种高效的检查点激酶 Chk1 和 WEE1 抑制剂（IC50 分别为 47 和 97 nM）。
T6084	Rabusertib LY2603618,IC-83	Chk; PDK; Autophagy	Autophagy; Cell Cycle/Checkpoint; PI3K/Akt/mTOR signaling
	Rabusertib (IC-83) 是一种有效的选择性的Chk1抑制剂，IC50为 7 nM。它有潜在的化学增强活性，用于各种癌症和肿瘤治疗的试验。
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。
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>。
T9252	LY2880070	Chk	Cell Cycle/Checkpoint
	LY2880070 是一种用于癌症治疗的新型检查点激酶 1 (CHK1) 抑制剂。
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。
T6077	ZM-447439	Apoptosis; MEK; Src; Aurora Kinase	Angiogenesis; Apoptosis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; MAPK; Tyrosine Kinase/Adaptors
	ZM 447439是一种极光激酶 (aurora) 抑制剂，对aurora A 和B 的IC50值分别为110和130 nM。
T10406	Tuvusertib M1774,ATR inhibitor 1	Apoptosis; ATM/ATR; Others; Chk	Apoptosis; Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Others; PI3K/Akt/mTOR signaling
	Tuvusertib (M1774) 是一种可口服的共济失调毛细血管扩张和 Rad3相关(ATR)激酶抑制剂(Ki< 1 µΜ)，具有选择性和潜在的抗肿瘤活性。Tuvusertib 选择性抑制 ATR 活性，阻断丝氨酸/苏氨酸蛋白激酶检查点激酶1 (CHK1)的下游磷酸化，从而抑制 DNA 损伤检查点激活，破坏 DNA 损伤修复，诱导肿瘤细胞凋亡。
T6532	Hesperadin	Influenza Virus; Parasite; Aurora Kinase; Autophagy	Autophagy; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Microbiology/Virology
	Hesperadin 是 Aurora A 和 B 的 ATP 竞争性吲哚酮抑制剂，抑制 Aurora B 的 IC50值为250nM。它通过阻断核分裂和胞质分裂而抑制布鲁氏锥虫的生长。它也是一种广谱流感抗病毒剂。
T5425	ML367	Epigenetic Reader Domain	Chromatin/Epigenetic
	ML367 是一种稳定的、有效的 ATPase 家族 AAA 结构域蛋白 5 抑制剂，是一个探针分子，具有低摩尔抑制浓度。它可以阻断 DNA 的修复通路，抑制一般的 DNA 损伤反应，包括应对紫外照射产生的 RPA32 和 CHK1 的磷酸化。
T14904	CCT244747	Chk	Cell Cycle/Checkpoint
	CCT244747 is a CHK1 inhibitor (IC50: 7.7 nM) and also abrogates G2 checkpoint (IC50: 29 nM).
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
T16141	MRT00033659	Others	Others
	MRT00033659 is an effective broad-spectrum kinase inhibitor of CK1 (IC50=0.9 µM for CK1δ) and CHK1 (IC50=0.23 µM). MRT00033659 is a pyrazolo-pyridine analogue. It also induces p53 pathway activation and E2F-1 destabilization.
T16848	SB-218078	Chk; PKC	Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling
	SB-218078 is less potently inhibits Cdc2 (IC50: 250 nM) and PKC (IC50: 1000 nM). SB-218078 is a potent, ATP-competitive, and cell-permeable checkpoint kinase 1 inhibitor that inhibits Chk1 phosphorylation of cdc25C (IC50: 15 nM).
T27424	GNE-783
	GNE-783 is a selective inhibitor of CHK1.
T24506	MU-380 MU 380,MU380
	MU-380 is an effective and selective inhibitor of CHK1.
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).
T70553	CCT245737(S)
	CCT245737(S) is a highly selective oral checkpoint kinase 1 (CHK1) inhibitor.
T23447	TCS 2312	Others	Others
	checkpoint kinase 1 (chk1) inhibitor
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.
T62735	GDC-0575 dihydrochloride
	GDC-0575 dihydrochloride (ARRY-575 dihydrochloride) 是一种选择性的、口服具有活力的 CHK1 抑制剂 (IC50: 1.2 nM)，表现出抗肿瘤效果。
T68981	PD-321852
	PD-321852 is a small-molecule Chk1 inhibitor, which potentiates gemcitabine-induced clonogenic death in a panel of pancreatic cancer cell lines and evaluated the relationship between endpoints associated with Chk1 inhibition and chemosensitization. Gemcitabine chemosensitization by minimally toxic concentrations of PD-321852 ranged from minimal (<3-fold change in survival) in Panc1 cells to >30-fold in MiaPaCa2 cells. PD-321852 inhibited Chk1 in all cell lines as evidenced by stabilization of Cd...
T10407	Gartisertib ATR inhibitor 2	ATM/ATR	DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling
	ATR inhibitor 2 is an orally active, ATP-competitive, and selective ATR inhibitor (Ki <150 pM) with antitumor activity. ATR inhibitor 2 potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (Chk1) phosphorylation (IC50: 8 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
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.
T9666	GDC-0425
	GDC-0425 (RG-7602) 是一种可口服的、高选择性的 ChK1抑制剂。GDC-0425 可用于多种恶性肿瘤的研究。
T83740	Ziptide TFA
	Ziptide是多种丝氨酸/苏氨酸蛋白激酶的肽底物，包括MAPK激活蛋白激酶2（MAPKAPK2）、MAPKAPK3、MAPKAPK5、checkpoint kinase 1（Chk1）、AMP激活蛋白激酶（AMPK）和钙/钙调蛋白依赖型蛋白激酶II（CamKII）。它被用来评估CamKII活性以用于抑制剂的开发。
T26981	Ceralasertib formate Ceralasertib,AZD-6738,AZD 6738,AZD6738
	Ceralasertib is an orally available inhibitor of ataxia telangiectasia and rad3 related (ATR) kinase. Ceralasertib selectively inhibits ATR activity by blocking the downstream phosphorylation of the serine/threonine protein kinase CHK1. This prevents ATR-
T69091	CBP501
	CBP501 is a peptide with G2 checkpoint-abrogating activity. G2 checkpoint inhibitor CBP501 inhibits multiple serine/threonine kinases, including MAPKAP-K2, C-Tak1, and CHK1, that phosphorylate serine 216 of the dual-specific phosphatase Cdc25C (cell division checkpoint 25 C); disruption of Cdc25C activity results in the inhibition of Cdc25C dephosphorylation of the mitotic cyclin-dependent kinase complex Cdc2/cyclin B, preventing entry into the mitotic phase of the cell cycle.
T10704	CCB02	Microtubule Associated	Cytoskeletal Signaling
	CCB02 是选择性的 CPAP-tubulin 相互作用抑制剂。CCB02能够与 tubulin 结合，竞争 β-tubulin 的 CPAP 结合位点，IC50 值为 689 nM，显示出高效的抗肿瘤活性。CCB02 对其他的蛋白没有抑制作用，包括中心体、细胞周期相关蛋白，对 Aurora A，Plk1，Plk2，CDK2 和 CHK1 的磷酸化状态也无作用。
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。

化合物

CHK1-IN-4 hydrochloride

Cat.No: T10792L

Synonym: CHK1-IN-4 hydrochloride（2120398-41-4 Free base）

Target: Chk

Cat.No: T10791

Target: Chk

Cat.No: T37098

Synonym: Chk1-IN-5

Cat.No: T40091

Synonym: Chk1-IN-6

Cat.No: T10790

Target: Chk

CHK1 inhibitor

Cat.No: T10793

Synonym: GDC-0575 analog

Target: Chk

Cat.No: T10792

Target: Chk

FLT3/CHK1-IN-1

Cat.No: T82393

Cat.No: T6028

Synonym: PF 00477736,PF-477736,PF-736,PF-00477736,PF477736

Target: c-Fms, VEGFR, FGFR, FLT, c-RET, Chk, CDK, Src, Aurora Kinase

Cat.No: T6931

Synonym: PD-166285

Target: Apoptosis, Wee1, Chk

Cat.No: T6093

Synonym: AZD7762

Target: Chk

Cat.No: T6350

Synonym: CHIR124,CHIR 124

Target: Apoptosis, GSK-3, FLT, Chk, PDGFR, Src

GDC0575 monohydrochloride

Cat.No: T27407

Synonym: ARRY-575,GDC-0575,GDC 0575,ARRY575,GDC0575

Target: Chk

Cat.No: T21331

Target: Chk

Cat.No: T7300

Synonym: ARRY-575,RG7741

Target: Chk

Cat.No: T2517

Synonym: MK 8776,MK-8776

Target: Chk, CDK

Cat.No: T7080

Synonym: SRA737

Target: Chk

Cat.No: T4310

Synonym: 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

Target: Apoptosis, Chk

Cat.No: T16446

Synonym: PD-407824

Target: Wee1, Chk

Cat.No: T6084

Synonym: LY2603618,IC-83

Target: Chk, PDK, Autophagy

SCH900776 (S-isomer)

Cat.No: T3700

Synonym: MK-8776 S-isomer,SCH900776 S-isomer

Target: Chk, CDK

Cat.No: T13148

Target: Chk

Cat.No: T71259

Synonym: GNE900,GNE 900

Target: Apoptosis, Chk

Cat.No: T9252

Target: Chk

Prexasertib dihydrochloride

Cat.No: T4327

Synonym: LY2606368 (dihydrochloride),Prexasertib HCl,LY2606368

Target: Apoptosis, Chk, S6 Kinase

Cat.No: T6077

Target: Apoptosis, MEK, Src, Aurora Kinase

Cat.No: T10406

Synonym: M1774,ATR inhibitor 1

Target: Apoptosis, ATM/ATR, Others, Chk

Cat.No: T6532

Target: Influenza Virus, Parasite, Aurora Kinase, Autophagy

Cat.No: T5425

Target: Epigenetic Reader Domain

Cat.No: T14904

Target: Chk

Prexasertib mesylate

Cat.No: T4310L2

Synonym: LY-2606368,LY2606368,LY 2606368

Cat.No: T16141

Target: Others

Cat.No: T16848

Target: Chk, PKC

Cat.No: T27424

Cat.No: T24506

Synonym: MU 380,MU380

CCT241533 hydrochloride

Cat.No: T10718L

Target: Chk

Cat.No: T70553

Cat.No: T23447

Target: Others

Prexasertib lactate hydrate

Cat.No: T4310L

Synonym: Prexasertib monolactate monohydrate,LY-2606368,LY 2606368,LY2606368,Prexasertib monolactate monohydrate salt

GDC-0575 dihydrochloride

Cat.No: T62735

Cat.No: T68981

Cat.No: T10407

Synonym: ATR inhibitor 2

Target: ATM/ATR

CCT241533 dihydrochloride

Cat.No: T36704

Synonym: CCT 241533 dihydrochloride

Prexasertib dimesylate

Cat.No: T38620

Synonym: LY2606368 dimesylate

Cat.No: T9666

Cat.No: T83740

Ceralasertib formate

Cat.No: T26981

Synonym: Ceralasertib,AZD-6738,AZD 6738,AZD6738

Cat.No: T69091

Cat.No: T10704

Target: Microtubule Associated

Cat.No: T33737

Synonym: NSC-109555,DDUG dimethanesulfonate,NSC109555,DDUG diMS

Cat. No.	Product Name	Target	Signaling Pathways
T3824	Jaceosidin	Apoptosis; BCL; COX; UGT	Apoptosis; Immunology/Inflammation; Metabolism; Neuroscience
	Jaceosidin 是从毛莲蒿中得到的一种黄酮类天然产物，可激活Bax，下调 Mcl-1 和 c-FLIP 的表达，诱导癌细胞凋亡。它能够降低炎性因子水平，激活 NF-κB，抑制COX-2的表达，具有抗癌和抗炎作用。

天然产物

Cat.No: T3824

Target: Apoptosis, BCL, COX, UGT

Species：

Expression System：

Tag：

Cat. No.	Product Name	Species	Expression System
TMPY-04368	Chk1 Protein, Human, Recombinant (GST) checkpoint kinase 1,CHK1	Human	Baculovirus Insect Cells
	Chk1 Protein, Human, Recombinant (GST) is expressed in Baculovirus insect cells with GST tag. The predicted molecular weight is 80.7kDa and the accession number is AAM78553.1.
TMPY-04433	Chk1 Protein, Mouse, Recombinant (His & GST) checkpoint kinase 1,Chk1,C85740,r...	Mouse	Baculovirus Insect Cells
	Chk1 Protein, Mouse, Recombinant (His & GST) is expressed in Baculovirus insect cells with His and GST tag. The predicted molecular weight is 82.2 kDa and the accession number is O35280-1.
TMPY-02228	p53 Protein, Cynomolgus, Recombinant tumor protein p53,p53,TP53	Cynomolgus	E. coli
	p53, also known as Tp53, is a DNA-binding protein which belongs to the p53 family. It contains transcription activation, DNA-binding, and oligomerization domains. p53 protein is expressed at low level in normal cells and at a high level in a variety of transformed cell lines, where it's believed to contribute to transformation and malignancy. p53 (TP53) is a transcription factor whose protein levels and post-translational modification state alter in response to cellular stress (such as DNA damag...

重组蛋白

Chk1 Protein, Human, Recombinant (GST)

Cat.No: TMPY-04368

Species: Human

Expression System: Baculovirus Insect Cells

Chk1 Protein, Mouse, Recombinant (His & GST)

Cat.No: TMPY-04433

Species: Mouse

Expression System: Baculovirus Insect Cells

p53 Protein, Cynomolgus, Recombinant

Cat.No: TMPY-02228

Species: Cynomolgus

Expression System: E. coli

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