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Search Results for " olaparib "

Targets Recommended: Mitophagy PARP Autophagy

抑制剂 & 化合物

同位素标记化合物

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Cat. No.	Product Name	Target	Signaling Pathways
T3015	Olaparib AZD2281,奥拉帕尼,KU0059436	Mitophagy; PARP; Autophagy	Autophagy; Chromatin/Epigenetic; DNA Damage/DNA Repair
	Olaparib (KU0059436) 是 PARP1/PARP2 的小分子抑制剂 (IC50=5/1 nM)，对 PARP tankyrase-1 的抑制活性较弱 (IC50=1.5 μM)，具有选择性和口服活性。Olaparib 具有自噬和线粒体自噬激活活性。
T36571	N-Descyclopropanecarbaldehyde Olaparib	Others	Others
	N-Descyclopropanecarbaldehyde Olaparib, an Olaparib analogue, incorporates a DOTA moiety. It acts as a CRBN-based ligand for the formation of novel dual EGFR and PARP PROTAC, DP-C-4[1]. N-Descyclopropanecarbaldehyde Olaparib is suitable for radiolabeling with F-18 or a fluorophore to visualize tumors using positron emission tomography (PET) or optical imaging[2].
T24597	PARPi-FL Olaparib-bodipy FL,Olaparib bodipy FL	Others	Others
	PARPi-FL is an agent of fluorescent PARP imaging. In vitro, it is capable of detecting the target engagement of a PARP inhibitor panel.
T63228	Simmiparib SMOCL-9112	Apoptosis; PARP	Apoptosis; Chromatin/Epigenetic; DNA Damage/DNA Repair
	Simmiparib (SMOCL-9112) 是一种新型有效的 PARP1 和 PARP2 抑制剂，是一种Olaparib 衍生物。Simmiparib 在同源重组修复 (HR) 缺陷细胞中诱导 DNA 双链断裂 (DSB) 和细胞周期阻滞，从而促使细胞凋亡 (apoptosis)。Simmiparib 可用于研究帕金森病、阿尔茨海默病、乳腺癌和黑色素瘤。
T68398	MI-223	Others	Others
	MI-223 is an inhibitor of Mcl-1-stimulated homologous recombination (HR) DNA repair, which leads to sensitization of cancer cells to hydroxyurea- or olaparib-induced DNA replication stress.
T61325	PARP1-IN-9	Others	Others
	PARP1-IN-9 (Compound 5c) is a potent PARP1 inhibitor, displaying an IC 50 of 30.51 nM. With its ability to induce cell apoptosis and exhibit anticancer activity, PARP1-IN-9 surpasses Olaparib in terms of efficacy [1].
T79667	YCH1899	PARP	Chromatin/Epigenetic; DNA Damage/DNA Repair
	YCH1899为一种口服活性PARP抑制剂，其对PARP1/2的IC50均低于0.001 nM。该化合物对Olaparib和Talazoparib耐药的Capan-1细胞株(Capan-1/OP及Capan-1/TP细胞)表现出显著抗增殖能力，IC50分别为0.89 nM和1.13 nM。在大鼠体内，YCH1899展现优良的药代动力学属性。
T36703	CAY10760	Others	Others
	CAY10760 is an inhibitor of the protein-protein interaction between RAD51 recombinase and BRCA2 (EC50= 19 μM in a cell-free competitive ELISA).1It decreases homologous recombination by 54% in wild-typeBRCA2-expressing BxPC-3 pancreatic cancer cells when used at a concentration of 20 μM. CAY10760 (20 μM) decreases proliferation of BxPC-3, as well as mutantBRCA2-expressing Capan-1, cancer cells when used alone or in combination with the poly(ADP-ribose) polymerase (PARP) inhibitor olaparib . 1.Bag...
T69931	MFH290	Others	Others
	MFH290 is a novel cysteine (Cys)-directed covalent inhibitor of CDK12/13. MFH290 forms a covalent bond with Cys-1039 of CDK12, exhibits excellent kinome selectivity, inhibits the phosphorylation of serine-2 in the C-terminal domain (CTD) of RNA-polymerase II (Pol II), and reduces the expression of key DNA damage repair genes. Importantly, these effects were demonstrated to be CDK12-dependent as mutation of Cys-1039 rendered the kinase refractory to MFH290 and restored Pol II CTD phosphorylation ...
T83854	BRC4wt TFA
	BRC4wt是一种从人类BRCA2的BRC4重复区(1521-1536)衍生而来的乙酰化肽，并且是BRCA2与RAD51之间的蛋白质-蛋白质相互作用的抑制剂。当与阳离子穿膜肽(Arg)9结合时，BRC4wt缩短了体外DNA复制轨迹长度，并降低了由DNA拓扑异构酶I抑制剂坎普特西汀引起的DNA损伤的同源修复频率，同时也增强了聚(ADP-核糖)聚合酶(PARP)抑制剂奥拉帕尼在HeLa人类宫颈癌细胞和U2OS人类骨肉瘤细胞中诱导的细胞死亡，但在非癌症细胞hTERT RPE-1、MRC-5或MCF-10A中则不然。

化合物

Olaparib

Cat.No: T3015

Synonym: AZD2281,奥拉帕尼,KU0059436

Target: Mitophagy, PARP, Autophagy

N-Descyclopropanecarbaldehyde Olaparib

Synonym: Olaparib-bodipy FL,Olaparib bodipy FL

Target: Others

Simmiparib

Cat.No: T63228

Synonym: SMOCL-9112

Target: Apoptosis, PARP

Cat. No.	Product Name	Target	Signaling Pathways
T12292	Olaparib-d5 KU0059436 D5,AZD2281 D5,Olaparib D5	Others	Others
	Olaparib D5 is a deuterium labeled Olaparib. Olaparib is a potent and oral inhibitor of PARP.

同位素标记化合物

Olaparib-d5

Cat.No: T12292

Synonym: KU0059436 D5,AZD2281 D5,Olaparib D5

Target: Others

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