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Search Results for " parp 2 in 1 "

28

抑制剂 & 化合物

4

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T12364	PARP-2-IN-1	Others	Others
	PARP-2-IN-1 is a potent and selective inhibitor of PARP-2(IC50 of 11.5 nM).
T72862	PARP-2/1-IN-2 ABT-888对映体
	PARP-2/1-IN-2 是 Veliparib 的对映异构体，是一种有效的PARP 抑制剂，对PARP-2和PARP-1的Ki 分别为 2 和 5 nM。在以PARP 活性为基础的细胞测定中，PARP-2/1-IN-2 的 EC50为 3 nM。
T62281	PARP-1-IN-2	PARP	Chromatin/Epigenetic; DNA Damage/DNA Repair
	PARP-1-IN-2 是一种有效且可透过血脑屏障的 PARP1 抑制剂（IC50： 149 nM）。PARP-1-IN-2 在细胞实验中对人肺腺癌上皮细胞系 A549 显示出显著的抗增殖活性。PARP-1-IN-2 可诱导 A549 细胞凋亡。
T40310	PARP/EZH2-IN-1 PARP/EZH2-IN-1
	PARP/EZH2-IN-1 is a novel compound that functions as a dual inhibitor for both PARP (IC50 6.87 nM) and EZH2 (IC50 36.51 nM), showing promising potential for the treatment of triple-negative breast cancer with wild-type BRCA.
T9891	PARP1-IN-8 N-(3-chlorophenyl)-3-(1-oxo-4-phenylphthalazin-2(1H)-yl)propanamide	PARP	Chromatin/Epigenetic; DNA Damage/DNA Repair
	PARP1-IN-8 (N-(3-chlorophenyl)-3-(1-oxo-4-phenylphthalazin-2(1H)-yl)propanamide) 是PARP1的有效抑制剂（IC50 = 97 nM）。
T72437	PARP1/2/TNKS1/2-IN-1	Apoptosis; PARP; Wnt/beta-catenin	Apoptosis; Chromatin/Epigenetic; Cytoskeletal Signaling; DNA Damage/DNA Repair; Stem Cells
	PARP1/2/TNKS1/2-IN-1 是一种多靶点抑制剂，抑制 PARP-1、PARP-2、TNKS1 和 TNKS2 。PARP1/2/TNKS1/2-IN-1 具有潜在的抗肿瘤活性，可诱导细胞凋亡。
T78787	PARP-1/2-IN-2	PARP	Chromatin/Epigenetic; DNA Damage/DNA Repair
	PARP-1/2-IN-2（Compound 12e）是一款抑制PARP1/2/CDK12的分子，IC50值分别为34、30和285 nM。该化合物阻碍DNA损伤修复过程，并能诱发细胞周期阻滞与细胞凋亡。此外，PARP-1/2-IN-2能够有效抑制三阴性乳腺癌（TNBC）细胞和异种移植瘤的增长。
T62508	PARP-1/2-IN-1
	PARP-1/2-IN-1是一种有效的 PARP-1 (IC50: 0.51 nM) 和 PARP-2 (IC50: 23.11 nM) 抑制剂。
T62540	PARP1/BRD4-IN-2
	PARP1/BRD4-IN-2 是一种有效的、选择性的 PARP1 (IC50: 197 nM) 和 BRD4 (IC50: 238 nM) 抑制剂。PARP1/BRD4-IN-2 能够抑制 DNA 损伤修复，阻滞 G0/G1 细胞周期转变，诱导细胞凋亡 (apoptosis)。PARP1/BRD4-IN-2 对 MDA-MB-468 小鼠异种移植瘤模型表现出抗肿瘤效果。PARP1/BRD4-IN-2 能够用于研究三阴性乳腺癌 (TNBC)。
T78157	PARP-1-IN-3	Apoptosis; PARP	Apoptosis; Chromatin/Epigenetic; DNA Damage/DNA Repair
	PARP-1-IN-3 是一种高效的 PARP-1 抑制剂，对 PARP-1 和 PARP-2 具有抑制作用， IC50 值分别为 0.25 nM 和 2.34 nM。PARP-1-IN-3 具有潜在的抗炎活性，促使细胞凋亡并使细胞周期停滞在 G2/M 期。PARP-1-IN-3 可用于研究与癌症相关的疾病。
T6768	AZ6102	PARP; Wnt/beta-catenin	Chromatin/Epigenetic; Cytoskeletal Signaling; DNA Damage/DNA Repair; Stem Cells
	AZ6102 是TNKS1和TNKS2双重抑制剂，IC50值分别为 3 和 1 nM，选择性是对 PARP 家族其他蛋白的 100 多倍，对 PARP1、PARP2 和 PARP6 的IC50值分别为 2.0、0.5 和大于 3 μM。
T22264	AZ9482	PARP	Chromatin/Epigenetic; DNA Damage/DNA Repair
	AZ9482 是一种选择性 PARP1/2/6的三重抑制剂，IC50值分别为 1 、1 和640 nM。
T71026	MC2050 HCl
	MC2050 is a potent PARP-1 inhibitor. The IC50 for inhibition of PARP-1 activity is 119 nM, compared to 1.8 μM for PARP-2. MC2050 inhibits apoptosis and blocks poly ADP-ribosylation of histone H1 in hydrogen peroxide treated SH-SY5Y neuroblastoma cells.
T64289	Rucaparib camsylate
	Rucaparib (AG014699) camsylate 是一种口服具有活力的 PARP 蛋白 (PARP-1、PARP-2 及 PARP-3) 抑制剂，对 PARP-1 的 Ki=1.4 nM。Rucaparib camsylate 是一种六磷酸己糖脱氢酶 (H6PD) 抑制剂。Rucaparib camsylate 具有潜力进行去势抵抗性前列腺癌 (CRPC) 的研究研究。
T61335	Rucaparib hydrochloride
	Rucaparib hydrochloride, also known as AG014699, is a powerful and orally active compound that inhibits PARP proteins including PARP-1, PARP-2, and PARP-3 with a Ki value of 1.4 nM for PARP1. Additionally, Rucaparib hydrochloride acts as a modest inhibitor of hexose-6-phosphate dehydrogenase (H6PD). This compound shows potential in research for castration-resistant prostate cancer (CRPC) [1] [2] [3] [4].
T63065	Rucaparib tartrate
	Rucaparib (AG014699) tartrate 是一种口服具有活力的 PARP 蛋白 (PARP-1, PARP-2 和 PARP-3) 抑制剂，作用于 PARP-1 (Ki: 1.4 nM)。Rucaparib tartrate 是一种六磷酸己糖脱氢酶 (H6PD) 抑制剂。Rucaparib tartrate 具有潜力用于去势抵抗性前列腺癌 (CRPC) 的研究。
T61657	Rucaparib acetate
	Rucaparib (AG014699) acetate is a highly effective oral inhibitor of PARP proteins, specifically targeting PARP-1, PARP-2, and PARP-3, with a Ki value of 1.4 nM for PARP1. Additionally, it exhibits inhibitory action on hexose-6-phosphate dehydrogenase (H6PD) to a moderate extent. Rucaparib acetate shows promise in the field of research for castration-resistant prostate cancer (CRPC). [1] [2] [3] [4]
T81543	PARP1-IN-17	PARP	Chromatin/Epigenetic; DNA Damage/DNA Repair
	PARP1-IN-17为一种选择性PARP-1抑制剂，其针对PARP-1的IC50为19.24 nM ，对PARP-2的IC50为32.58 nM ，能够有效诱导(apoptosis)。此外，PARP1-IN-17显示出优秀的抗增殖作用。
T69955	JPI-547 HCl
	JPI 547, also known as NOV 1402, is an oral inhibitor of PARP 1/2 and Tankyrase 1/2. JPI-547 demonstrated anti-tumor activity in BRCA-deficient xenograft models as a single-agent and in combination with chemotherapy and immune checkpoint inhibitors.
T81541	PARP7-IN-16	PARP	Chromatin/Epigenetic; DNA Damage/DNA Repair
	PARP7-IN-16是一种高效、选择性且具有口服生物活性的PARP-1/2/7抑制剂，其IC50分别为0.94 nM , 0.87 nM 和0.21 nM 。PARP7-IN-16适合用于乳腺癌与前列腺癌的研究。
T78401	pNP-ADPr disodium ADP-ribose-pNP disodium
	pNP-ADPr 二钠是一种用于检测Poly(ADP-ribose) glycohydrolase (PARG)和ADP-ribosyl hydrolase 3 (ARH3)活性的比色底物。它也适用于poly(ADP-ribose)polymerase (PARP)酶相关研究。
T72017	6(5H)-Phenanthridinone
	6(5H)-Phenanthridinone is an inhibitor of poly(ADP-ribose) polymerase 1 (PARP1) and PARP2. It decreases radiation-induced PARP activity and proliferation of RDM4 murine lymphoma cells. 6(5H)-Phenanthridinone reduces NF-κB-induced transcription of the genes encoding TNF-α, IL-2, and IFN-γ in rat lymphocytes. In vivo, 6(5H)-phenanthridinone reduces spinal cord expression of inducible nitric oxide synthase (iNOS), IL-1β, TNF-α, IL-2, and IFN-γ and reduces disease score in a rat model of experimenta...
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。
T70138	AZ0108
	AZ0108 is an orally bioavailable, potent PARP1,2,6 inhibitor that potently inhibits centrosome clustering and is suitable for in vivo efficacy and tolerability studies. AZ0108 has been utilized as in vitro tools and in vivo probes to investigate the biological consequences of inhibiting centrosome clustering through PARP enzymes. AZ0108 is more selective in its enzyme inhibition profile and effects on cellular pathways and phenotypes. Specifically, AZ0108 inhibits PARPs 1, 2, and 6 with approxi...
T75074	6-Methoxypurine-9-β-D-5’(R)-C-methylriboside
	6-Methoxypurine-9-β-D-5’(R)-C-methylriboside 是一种嘌呤碱基，属于次黄嘌呤似物，主要在肌肉组织中发现。作为黄嘌呤在嘌呤氧化酶作用下的代谢产物，次黄嘌呤具备显著的抗炎性质，并可作为内源性 poly(ADP-ribose) polymerase (PARP) 的抑制剂。其通过抑制 PARP 活性，防止过氧亚硝酸盐引起的线粒体去极化及次级超氧化物的产生，展现出细胞保护作用。同时，次黄嘌呤也被用作缺氧的生物标志物。
T71757	SC-10914
	SC10914 is a highly potent PARP inhibitor (PARP1 IC50 = 7.87 nM) with potent anti-proliferative activity against human BRCA deficient tumor cells (MDA-MB-436, BRCA1 deficient, IC50 = 4.03 nM, Capan-1 BRCA2 deficient, IC50 = 11.66 nM) and PTEN deficient tumor cells (HGC-27,PTEN deficient, IC50 = 0.35 μM). SC10914 showed potent anti-tumor activity in BRCA1/2 mutant tumor models and better pharmacokinetics profile has the potential to be selected as the clinical candidate for the treatment of treat...
T72554	ARTD10/PARP10-IN-2
	ARTD10/PARP10-IN-2 是一种强效、非选择性的PARP 抑制剂。ARTD10/PARP10-IN-2 靶向单 ADP 核糖转移酶 (ARTD10/PARP10) 和聚 ADP-核糖聚合酶-1 (ARTD1/PARP1)，IC50分别为 2.0 μM，和 9.7 μM。
T71230	VMY-1-103
	VMY-1-103 is a potent CDK inhibitor, is also a novel dansylated analog of purvalanol B, was shown to inhibit cell cycle progression and proliferation in prostate and breast cancer cells more effectively than purvalanol B. VMY-1-103 , but not purvalanol B, significantly decreased the proportion of cells in S phase and increased the proportion of cells in G(2)/M. VMY-1-103 increased the sub G(1) fraction of apoptotic cells, induced PARP and caspase-3 cleavage and increased the levels of the Death ...

化合物

Cat.No: T12364

Target: Others

PARP-2/1-IN-2

Cat.No: T72862

Synonym: ABT-888对映体

Cat.No: T62281

Target: PARP

PARP/EZH2-IN-1

Cat.No: T40310

Synonym: PARP/EZH2-IN-1

Cat.No: T9891

Synonym: N-(3-chlorophenyl)-3-(1-oxo-4-phenylphthalazin-2(1H)-yl)propanamide

Target: PARP

PARP1/2/TNKS1/2-IN-1

Cat.No: T72437

Target: Apoptosis, PARP, Wnt/beta-catenin

PARP-1/2-IN-2

Cat.No: T78787

Target: PARP

PARP-1/2-IN-1

Cat.No: T62508

PARP1/BRD4-IN-2

Cat.No: T62540

Cat.No: T78157

Target: Apoptosis, PARP

Cat.No: T6768

Target: PARP, Wnt/beta-catenin

Cat.No: T22264

Target: PARP

Cat.No: T71026

Rucaparib camsylate

Cat.No: T64289

Rucaparib hydrochloride

Cat.No: T61335

Rucaparib tartrate

Cat.No: T63065

Rucaparib acetate

Cat.No: T61657

Cat.No: T81543

Target: PARP

Cat.No: T69955

Cat.No: T81541

Target: PARP

pNP-ADPr disodium

Cat.No: T78401

Synonym: ADP-ribose-pNP disodium

6(5H)-Phenanthridinone

Cat.No: T72017

Cat.No: T79667

Target: PARP

Cat.No: T70138

6-Methoxypurine-9-β-D-5’(R)-C-methylriboside

Cat.No: T75074

Cat.No: T71757

ARTD10/PARP10-IN-2

Cat.No: T72554

Cat.No: T71230

Cat. No.	Product Name	Target	Signaling Pathways
T5S2358	Dehydrocorydaline Dehydrocorydalin,脱氢紫堇碱,13-Methylpalmatine	BCL; PARP; p38 MAPK; Caspase; Parasite; Autophagy	Apoptosis; Autophagy; Chromatin/Epigenetic; DNA Damage/DNA Repair; MAPK; Microbiology/Virology; Proteases/Proteasome
	Dehydrocorydaline (13-Methylpalmatine) 是一种生物碱。它调节Bax，Bcl-2蛋白表达，激活caspase-7，caspase-8，并使PARP 失活。它能增强p38 MAPK 活化，具有抗炎、抗癌等功效。它具有强大的抗疟疾作用，并具低细胞毒性。
T3S1471	Cucurbitacin IIA 葫芦素Iia,Dihydrocucurbitacin Q1,Hemslecin A,Curcurbitacin IIA	Apoptosis; Survivin	Apoptosis
	Cucurbitacin IIA (Dihydrocucurbitacin Q1) 是从园果雪胆中分离得到的一种三萜烯，可诱导细胞凋亡和增强自噬，有助于葫芦素IIA 对炎症相关疾病的抗炎活性。它可降低癌细胞中生存素的表达，降低磷酸化组蛋白 H3 的水平，增加裂解的 PARP 的水平。
T2S2362	Dehydrocorydaline nitrate 去氢延胡索甲素硝酸盐,硝酸脱氢紫堇碱	BCL; Others; PARP; p38 MAPK; Caspase; Parasite; Autophagy	Apoptosis; Autophagy; Chromatin/Epigenetic; DNA Damage/DNA Repair; MAPK; Microbiology/Virology; Others; Proteases/Proteasome
	Dehydrocorydaline nitrate 是生物碱。Dehydrocorydaline 调节 Bax，Bcl-2蛋白表达，激活 caspase-7，caspase-8，并使 PARP 失活。它能增强 p38 MAPK 活化，具有抗炎、抗癌、抗疟疾等功效。
T5S1805	5,7-Dihydroxychromone 5,7-Dihydroxy-4H-Chromen-4-One,5,7-二羟基色酮,5,7-二羟基色原酮	Others; Virus Protease; PARP; Caspase; Nrf2	Apoptosis; Chromatin/Epigenetic; DNA Damage/DNA Repair; Immunology/Inflammation; Microbiology/Virology; Others; Proteases/Proteasome
	5,7-Dihydroxychromone (5,7-Dihydroxy-4H-Chromen-4-One) 是一种Cudrania tricuspidata 的提取物，通过激活 Nrf2/ARE 信号对 6-OHDA 诱导的氧化应激和细胞凋亡发挥神经保护作用。它抑制 6-OHDA 诱导的 SH-SY5Y 细胞中活化的caspase-3，caspase-9以及切割的PARP 表达。

天然产物

Dehydrocorydaline

Cat.No: T5S2358

Synonym: Dehydrocorydalin,脱氢紫堇碱,13-Methylpalmatine

Target: BCL, PARP, p38 MAPK, Caspase, Parasite, Autophagy

Cucurbitacin IIA

Cat.No: T3S1471

Synonym: 葫芦素Iia,Dihydrocucurbitacin Q1,Hemslecin A,Curcurbitacin IIA

Target: Apoptosis, Survivin

Dehydrocorydaline nitrate

Cat.No: T2S2362

Synonym: 去氢延胡索甲素硝酸盐,硝酸脱氢紫堇碱

Target: BCL, Others, PARP, p38 MAPK, Caspase, Parasite, Autophagy

5,7-Dihydroxychromone

Cat.No: T5S1805

Synonym: 5,7-Dihydroxy-4H-Chromen-4-One,5,7-二羟基色酮,5,7-二羟基色原酮

Target: Others, Virus Protease, PARP, Caspase, Nrf2

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