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19

抑制剂 & 化合物

5

天然产物

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Cat. No. Product Name Target Signaling Pathways
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。
T6329 3-Aminobenzamide

3-AB,INO1001,INO-1001,3-ABA,PARP-IN-1,INO 1001

PARP Chromatin/Epigenetic; DNA Damage/DNA Repair
3-Aminobenzamide (PARP-IN-1) 是一种有效的 PARP 抑制剂,在 CHO 细胞中,对 PARP 的 IC50值约为 50 nM。它是再灌注过程中氧化剂诱导的肌细胞功能障碍的介质。
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)。
T12365 PARP/PI3K-IN-1

PARP; PI3K Chromatin/Epigenetic; DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling
PARP/PI3K-IN-1 是一种 新型双重聚(ADP-核糖)聚合酶(PARP)和磷酸肌醇 3-激酶(PI3K)双重抑制剂,具有抗癌、抗肿瘤和抗癌细胞增殖活性,可用于研究乳腺癌、胰腺癌和肺癌。
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 31 nM,选择性是对 PARP 家族其他蛋白的 100 多倍,对 PARP1PARP2 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 11 和640 nM。
T10896L CSRM617 hydrochloride

CSRM617 hydrochloride(787504-88-5 Free base)

Apoptosis; Others; Androgen Receptor Apoptosis; Endocrinology/Hormones; Others
CSRM617 hydrochloride 是转录因子ONECUT2(OC2,雄激素受体 AR 的主要调节剂) 的选择性小分子抑制剂,在 SPR 测定中Kd 为 7.43 uM,直接与 OC2-HOX 结构域结合。CSRM617 hydrochloride 通过裂解 Caspase-3PARP 诱导细胞凋亡 (apoptosis)。CSRM617 hydrochloride 在小鼠的前列腺癌模型中具有良好的耐受性。
T64289 Rucaparib camsylate

Rucaparib (AG014699) camsylate 是一种口服具有活力的 PARP 蛋白 (PARP-1PARP-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。
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。
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].
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]
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。
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。
T79791 Immunosuppressant-1

Apoptosis Apoptosis
Immunosuppressant-1(Compound 31)抑制抗-CD3/抗-CD28共刺激的T细胞增殖,具备免疫抑制活性。该化合物能激活活化的淋巴结细胞中的caspase-3PARP,从而诱导细胞凋亡(apoptosis)。
T79482 Anticancer agent 137

PI3K PI3K/Akt/mTOR signaling
Anticanceragent 137 (8q) 是一种高效的 PI3k 抑制剂,展现出广谱的抗肿瘤活性。它能够诱导 G2/M 阶段的细胞周期阻滞与细胞凋亡(apoptosis),并促进 PARP、caspase 3 和 caspase 7 的裂解。该化合物主要用于癌症相关的生物医学研究。
T36703 CAY10760

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...
T63522 Anticancer agent 64

Anticancer agent 64 (化合物 5m) 对 CCRF-CEM 细胞具有细胞毒性,其IC50为2.4 μM。Anticancer agent 64 通过诱导细胞凋亡表现出良好的抗癌活性。Anticancer agent 64 诱导caspase 3和 7 的激活和PARP 的裂解。Anticancer agent 64 具有明显的线粒体去极化作用。
T79713 JMJD3/HDAC-IN-1

HDAC Chromatin/Epigenetic; DNA Damage/DNA Repair
JMJD3/HDAC-IN-1 (compound A5b) 是靶向 JMJD3 和 HDAC1(IC50=16 nM)的双重抑制剂。它能够促进 H3K27 高甲基化和 H3K9 高乙酰化,并通过裂解 caspase-7 和 PARP 导致细胞凋亡。此外,JMJD3/HDAC-IN-1 对抑制癌细胞克隆形成、迁移和侵袭也表现出有效性。
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

PARP-1-IN-3
Cat.No: T78157
Synonym:
Target: Apoptosis, PARP
3-Aminobenzamide
Cat.No: T6329
Synonym: 3-AB,INO1001,INO-1001,3-ABA,PARP-IN-1,INO 1001
Target: PARP
PARP1-IN-8 
Cat.No: T9891
Synonym: N-(3-chlorophenyl)-3-(1-oxo-4-phenylphthalazin-2(1H)-yl)propanamide
Target: PARP
PARP/PI3K-IN-1
Cat.No: T12365
Synonym:
Target: PARP, PI3K
AZ6102
Cat.No: T6768
Synonym:
Target: PARP, Wnt/beta-catenin
AZ9482
Cat.No: T22264
Synonym:
Target: PARP
CSRM617 hydrochloride
Cat.No: T10896L
Synonym: CSRM617 hydrochloride(787504-88-5 Free base)
Target: Apoptosis, Others, Androgen Receptor
Rucaparib camsylate
Cat.No: T64289
Synonym:
Target:
PARP-2/1-IN-2
Cat.No: T72862
Synonym: ABT-888对映体
Target:
Rucaparib hydrochloride
Cat.No: T61335
Synonym:
Target:
Rucaparib acetate
Cat.No: T61657
Synonym:
Target:
Rucaparib tartrate
Cat.No: T63065
Synonym:
Target:
pNP-ADPr disodium
Cat.No: T78401
Synonym: ADP-ribose-pNP disodium
Target:
Immunosuppressant-1
Cat.No: T79791
Synonym:
Target: Apoptosis
Anticancer agent 137
Cat.No: T79482
Synonym:
Target: PI3K
CAY10760
Cat.No: T36703
Synonym:
Target:
Anticancer agent 64
Cat.No: T63522
Synonym:
Target:
JMJD3/HDAC-IN-1
Cat.No: T79713
Synonym:
Target: HDAC
VMY-1-103
Cat.No: T71230
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
TN1880 Lucidenic acid B

Lucidenicacid B

Apoptosis; Caspase Apoptosis; Proteases/Proteasome
Lucidenic acid B (Lucidenicacid B) 是从灵芝中提取得到的天然化合物,可诱导caspase-9 和 caspase-3 的活化和 PARP 的裂解,可通过线粒体介导诱导人白血病细胞凋亡 。 Lucidenic acid B通过灭活MAPK / ERK信号转导途径和降低NF-kappaB和AP-1的结合活性来抑制PMA诱导的人肝癌细胞侵袭。。Lucidenic acid B 对细胞周期和坏死细胞没有影响。
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。
T6S2391 L-Chicoric Acid

(-)-Chicoric acid,trans-Caffeoyltartaric acid,Chicoric acid,L-菊苣酸,dicaffeoyltartaric acid,菊苣酸

Others; HIV Protease Microbiology/Virology; Others; Proteases/Proteasome
L-Chicoric Acid (trans-Caffeoyltartaric acid) 是一种二咖啡酰酒石酸,是一种选择性可逆的 HIV-1 整合酶抑制剂,IC50约为 100 nM。它还可抑制 HIV-1 复制。
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

Lucidenic acid B
Cat.No: TN1880
Synonym: Lucidenicacid B
Target: Apoptosis, Caspase
Dehydrocorydaline
Cat.No: T5S2358
Synonym: Dehydrocorydalin,脱氢紫堇碱,13-Methylpalmatine
Target: BCL, PARP, p38 MAPK, Caspase, Parasite, Autophagy
L-Chicoric Acid
Cat.No: T6S2391
Synonym: (-)-Chicoric acid,trans-Caffeoyltartaric acid,Chicoric acid,L-菊苣酸,dicaffeoyltartaric acid,菊苣酸
Target: Others, HIV Protease
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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