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Search Results for " chk1 inhibitor "

48

抑制剂 & 化合物

1

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T10793	CHK1 inhibitor GDC-0575 analog	Chk	Cell Cycle/Checkpoint
	CHK1 inhibitor (GDC-0575 analog) is a CHK1 inhibitor.
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。
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。
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。
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。
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。
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。
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。
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。
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。
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。
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。
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。
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）。
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。
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。
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>。
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。
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。
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。
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).
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.
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
T23447	TCS 2312	Others	Others
	checkpoint kinase 1 (chk1) inhibitor
T70553	CCT245737(S)
	CCT245737(S) is a highly selective oral checkpoint kinase 1 (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.
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.
T14904	CCT244747	Chk	Cell Cycle/Checkpoint
	CCT244747 is a CHK1 inhibitor (IC50: 7.7 nM) and also abrogates G2 checkpoint (IC50: 29 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].
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).
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).
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...
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。
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-
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
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。
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。
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。
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.
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.
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。
T81740	Multi-kinase-IN-6	Trk receptor	Tyrosine Kinase/Adaptors
	Multi-kinase-IN-6 (compound 10e) 是一种效能极高的多激酶抑制剂，具有对 TrkA、ALK2、c-KIT、EGFR、PIM1、CK2α、CHK1 和 CDK2 等多种酶的显著抑制作用。在 MCF7、HCT116 和 EKVX 癌细胞系上，其抗增殖活性突出，IC50 值分别达到 3.36 μM、1.40 μM 与 3.49 μM。此外，Multi-kinase-IN-6 能引起 MCF7 与 HCT116 细胞的细胞周期在 G1/S 期及 G1 期停滞，并有效诱导凋亡。

化合物

CHK1 inhibitor

Cat.No: T10793

Synonym: GDC-0575 analog

Target: Chk

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

CHK1-IN-4 hydrochloride

Cat.No: T10792L

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

Target: Chk

Cat.No: T6931

Synonym: PD-166285

Target: Apoptosis, Wee1, Chk

Cat.No: T10791

Target: Chk

Cat.No: T13148

Target: Chk

Cat.No: T9252

Target: Chk

Cat.No: T6093

Synonym: AZD7762

Target: Chk

Cat.No: T7300

Synonym: ARRY-575,RG7741

Target: Chk

Cat.No: T6350

Synonym: CHIR124,CHIR 124

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

Cat.No: T7080

Synonym: SRA737

Target: Chk

Cat.No: T21331

Target: Chk

GDC0575 monohydrochloride

Cat.No: T27407

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

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

SCH900776 (S-isomer)

Cat.No: T3700

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

Target: Chk, CDK

Cat.No: T6084

Synonym: LY2603618,IC-83

Target: Chk, PDK, Autophagy

Cat.No: T71259

Synonym: GNE900,GNE 900

Target: Apoptosis, Chk

Cat.No: T6077

Target: Apoptosis, MEK, Src, Aurora Kinase

Cat.No: T10406

Synonym: M1774,ATR inhibitor 1

Target: Apoptosis, ATM/ATR, Others, Chk

Prexasertib dihydrochloride

Cat.No: T4327

Synonym: LY2606368 (dihydrochloride),Prexasertib HCl,LY2606368

Target: Apoptosis, Chk, S6 Kinase

Cat.No: T5425

Target: Epigenetic Reader Domain

Cat.No: T40091

Synonym: Chk1-IN-6

Cat.No: T10790

Target: Chk

Cat.No: T27424

Cat.No: T24506

Synonym: MU 380,MU380

Prexasertib mesylate

Cat.No: T4310L2

Synonym: LY-2606368,LY2606368,LY 2606368

Cat.No: T23447

Target: Others

Cat.No: T70553

Cat.No: T10792

Target: Chk

Prexasertib lactate hydrate

Cat.No: T4310L

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

Cat.No: T14904

Target: Chk

Cat.No: T37098

Synonym: Chk1-IN-5

Cat.No: T16141

Target: Others

Cat.No: T16848

Target: Chk, PKC

Cat.No: T10407

Synonym: ATR inhibitor 2

Target: ATM/ATR

GDC-0575 dihydrochloride

Cat.No: T62735

Cat.No: T68981

Cat.No: T9666

Ceralasertib formate

Cat.No: T26981

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

CCT241533 dihydrochloride

Cat.No: T36704

Synonym: CCT 241533 dihydrochloride

FLT3/CHK1-IN-1

Cat.No: T82393

Cat.No: T33737

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

Cat.No: T10704

Target: Microtubule Associated

Cat.No: T69091

Prexasertib dimesylate

Cat.No: T38620

Synonym: LY2606368 dimesylate

Prexasertib Mesylate Hydrate

Cat.No: T63152

Multi-kinase-IN-6

Cat.No: T81740

Target: Trk receptor

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

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