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39

抑制剂 & 化合物

2

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Cat. No. Product Name Target Signaling Pathways
T5399 GeA-69

PARP Chromatin/Epigenetic; DNA Damage/DNA Repair
GeA-69 是一种选择性变构 PARP14 大结构域 2 (MD2) 抑制剂,Kd 值为 2.1 µM。
T7318 Elimusertib

BAY-1895344

ATM/ATR DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling
Elimusertib (BAY-1895344) 是一种可口服的选择性ATR 抑制剂,IC50值为 7 nM。它具有抗肿瘤活性,可研究实体瘤和淋巴瘤。
T23974 DDRI-18

DDRI18,DDRI 18

DNA/RNA Synthesis Cell Cycle/Checkpoint; DNA Damage/DNA Repair
DDRI-18 是一种调节 DNA 损伤反应的新型小分子抑制剂,具有增敏活性和抗癌活性,抑制非同源末端连接 (NHEJ) DNA 修复过程,增强抗癌 DNA 损伤化合物的细胞毒性作用。
T12682 Emzadirib

CYT-0851,RAD51-IN-2

DNA/RNA Synthesis Cell Cycle/Checkpoint; DNA Damage/DNA Repair
Emzadirib (RAD51-IN-2) 是一种有效的 RAD51 抑制剂,具有潜在的抗癌活性,可用于研究 DNA 损伤修复。
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。
T3231 Niraparib

尼拉帕尼,MK-4827

Apoptosis; Others; PARP Apoptosis; Chromatin/Epigenetic; DNA Damage/DNA Repair; Others
Niraparib (MK-4827) 是一种 PARP 抑制剂,可以抑制 PARP1 和 PARP2 (IC50=3.8/2.1 nM),具有选择性。Niraparib 具有抗肿瘤活性,可以抑制 DNA 损伤修复、诱导细胞凋亡。
T50098 TIQ-A

PARP Chromatin/Epigenetic; DNA Damage/DNA Repair
TIQ-A 是一种 PARP1 抑制剂,通过碱基切除修复途径参与 DNA 单链断裂修复。 PARP1 由 DNA 损伤触发,其过度激活已被认为是许多病理状况的致病因素,包括缺血和再灌注损伤、哮喘相关炎症和动脉粥样硬化形成。
T70873 M3541

Apoptosis; ATM/ATR Apoptosis; DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling
M3541 是一种具有选择性有效性和口服活性的 ATM 抑制剂,具有潜在抗肿瘤活性。M-3541 通过与 ATM 结合来抑制 ATM 的激酶活性和 ATM 介导的信号传导。M3541 防止 DNA 损伤检查点激活,抑制 DNA 损伤修复,促使肿瘤细胞凋亡,并诱导 ATM 过表达的肿瘤细胞死亡。
T21320 Methoxyamine HCl

甲氧基胺盐酸盐,TRC102,TRC 102,Methoxyamine,TRC-102

Others Others
Methoxyamine HCl (Methoxyamine) 与脱嘌呤/脱嘧啶 (AP) DNA 损伤位点共价结合并抑制碱基切除修复 (BER),这可能导致 DNA 链断裂和细胞凋亡增加。 Methoxyamine 是一种具有潜在佐剂活性的口服生物可利用的小分子抑制剂。该药剂可增强烷化剂的抗肿瘤活性。
T25838 MS0017509

MS-0017509,MS 0017509

MS0017509 is a DNA damage repair inhibitor.
T25839 MS0019266

MS 0019266,MS-0019266

MS0019266 is a DNA damage repair inhibitor.
T69931 MFH290

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 ...
T40345 AV-153

AV-153 is a 1,4-dihydropyridine derivative with antimutagenic properties. It intercalates into DNA at single strand breaks, resulting in reduced DNA damage and stimulation of DNA repair in human cells in vitro. AV-153 also interacts with thymine and cytosine and influences poly(ADP)ribosylation. Moreover, AV-153 exhibits anti-cancer activity.
T80207 Tetrapeptide

DNA/RNA Synthesis Cell Cycle/Checkpoint; DNA Damage/DNA Repair
Tetrapeptide 作为α-MSH的类似物,能促进黑色素的合成;其通过降低活性氧化物质生成和提升DNA光产物修复效率,有效减轻DNA损伤。
T81140 SNM1A-IN-1

SNM1A-IN-1(化合物11a)是一种针对SNM1A(一种具备细胞毒性的DNA损伤修复酶)的抑制剂。
T63923 ATR-IN-5

ATR-IN-5 是 ATR 的有效抑制剂。其中 ATR 是 PIKK 家族的成员,是一类参与基因组稳定性和 DNA 损伤修复的蛋白激酶。ATR-IN-5 对 ATR 激酶介导的疾病如增殖性疾病和癌症表现出研究潜力。
T36701 Phosphoramide mustard (cyclohexanamine)

Phosphoramide mustard cyclohexanamine is the major metabolite for Cyclophosphamide , with anticancer activitiy. Phosphoramide mustard cyclohexanamine induces DNA adduct formation in ovarian granulosa cells, induces DNA damage and elicits the ovarian DNA repair response[1][2]. Phosphoramide mustard cyclohexanamine causes cytotoxicity through forming cross-linked DNA adducts which inhibit DNA strand separation during replication[1].Phosphoramide mustard cyclohexanamine destroys rapidly dividing ce...
T14282 Amuvatinib hydrochloride

HPK 56 hydrochloride,MP470 hydrochloride

Others Others
Amuvatinib hydrochloride (MP470 hydrochloride) is an orally bioavailable multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Kit, PDGFRα, Flt3, c-Met and c-Ret and is also a DNA repair suppressor through suppression of DNA repai
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-
T78581 Selenocystine

Others Others
Selenocystine为一种广谱抗癌剂,能诱导HepG2细胞发生DNA损伤,尤其是 DNA 双链断裂(DSBs)。Selenocystine在靶向DNA修复领域,作为癌症治疗的潜在治疗或辅助剂,展现出显著的应用前景。
T40931 FEN1-IN-2

Others Others
FEN1-IN-2 是一种具有选择性和有效性的瓣内切酶 1 (FEN1) 的抑制剂,抑制 FEN1 和 XPG,具有潜在的抗癌活性,可用于研究DNA损伤修复。
T32189 Iproplatin

JM-9,CHIP,Code name: JM9,JM 9

Iproplatin is a synthetic second-generation platinum-containing compound related to cisplatin. Iproplatin binds to and forms DNA crosslinks and platinum-DNA adducts, resulting in DNA replication failure and cell death. Although less prone to glutathione i
T81249 Ru3

PARP Chromatin/Epigenetic; DNA Damage/DNA Repair
Ru3是一种poly(ADP-ribose)polymerase 1抑制剂,能够通过诱导DNA损伤、抑制DNA修复机制、扰乱细胞周期、降低线粒体膜电位及增加reactive oxygen species水平来诱导MCF-7细胞的apoptosis。
T75335 Ethylenediaminetetraacetic acid dipotassium dihydrate

Ethylenediaminetetraacetic acid (EDTA) dipotassium dihydrate 是抗凝血剂,可螯合重金属,解除毒性。Ethylenediaminetetraacetic acid dipotassium dihydrate 可破坏染色体、干扰 DNA 修复过程,增加减数分裂交换的发生率。
T81640 NSC15520

NSC15520是一种小分子RPA抑制剂,特异性结合RPA的N端DNA结合域(DBD),阻断其与p53或RAD9的相互作用。它还能够抑制双链DNA(dsDNA)寡核苷酸的螺旋不稳定性,影响DNA复制、修复、重组及损伤反应信号。
T75021 SZUH280

SZUH280 是一种有效的、选择性的 PROTACHDAC8降解剂,在 A549 细胞中的 DC50为 0.58 μM。SZUH280 诱导癌细胞凋亡 (apoptosis)。SZUH280 在癌细胞中阻碍 DNA 损伤修复,促进细胞放射致敏。
T70978 5-Hydroxy Lansoprazole Sulfide

5-Hydroxy Lansoprazole Sulfide is an inhibitor of fatty acid synthase (FASN). FASN, which is responsible for de-novo synthesis of lipids, has been found to be overexpressed in cancerous tissue. 5-Hydroxy Lansoprazole Sulfide specifically inhibits enoyl reductase, and was found to more effectively inhibit FASN function than lansoprazole and was also more efficient at regulating NHEJ repair of oxidative DNA damage via PARP1.
T37729 IMP-1700

IMP-1700 is an inhibitor of bacterial DNA repair.1It potentiates the activity of the quinolone antibiotic ciprofloxacin against methicillin-resistantS. aureus(MRSA) with a combination index value of 0.7. IMP-1700 inhibits the ciprofloxacin-induced bacterial SOS response, a process that repairs DNA damage, in a reporter assay in a concentration-dependent manner. It is also active againstE. coli, as well as methicillin-resistant and -sensitive S. aureus, when used alone (EC50s = 0.5, 0.21, and 3.8...
T73299 APE1-IN-2

Apoptosis Apoptosis
APE1-IN-2(compound AP1)是一种具有抗癌活性的Pt(IV)前体,靶向BER关键蛋白APE1。该化合物能诱导细胞内铂的积累,并激活DNA损伤反应及凋亡信号。
T60649 AV-153 free base

AV-153 free base 是一种 1,4-二氢吡啶(1,4-DHP) 衍生物。AV-153 free base 是一种抗诱变剂,具有抗癌活性。AV-153 free base 可以与胞嘧啶和胸腺嘧啶相互作用,并影响聚 (ADP) 核糖基化。在体外实验中,AV-153 free base 在 DNA 的单链断裂处插入到 DNA 并减少 DNA 损伤,刺激 DNA 修复。
T79134 FEN1-IN-6

FLAP Immunology/Inflammation
FEN1-IN-6(化合物9)是一种高效的Flap内切酶1(FEN1,IC50=10 nM)抑制剂,对哺乳动物细胞DNA损伤修复有关键作用。同时,FEN1-IN-6也针对相关酶,如XPG,表现出较强的抑制活性(IC50为23 nM)。
T63555 ATR-IN-6

ATR-IN-6 是 ATR 的有效抑制剂。其中 ATR 是一种蛋白激酶,能够参与基因组稳定性和 DNA 损伤修复,是 PIKK 家族的成员。ATR-IN-6 对 ATR 激酶介导的疾病如增殖性疾病和癌症表现出研究潜力。
T79135 FEN1-IN-7

FLAP Immunology/Inflammation
FEN1-IN-7(化合物16)是一款选择性Flap内切酶1(FEN1,IC50=18 nM)抑制剂,它在哺乳动物细胞的DNA损伤修复过程中发挥作用。此外,FEN1-IN-7对相关内切酶如着色性干皮病G蛋白(XPG,IC50=3.04 μM)也有靶向性。它能提高癌细胞对DNA烷基化剂或甲基化试剂的敏感性。
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。
T78138 SIC5-6

Others Others
SIC5-6为一强效Separase抑制剂,此酶为大型半胱氨酸蛋白酶,关键参与有丝分裂与减数分裂中染色体分离,DNA损伤修复,中心体分离与复制,以及纺锤体稳定与伸长。Separase在众多实体瘤高表达,成为潜在的化疗靶标。
T79689 SIRT6-IN-3

Sirtuin Chromatin/Epigenetic; DNA Damage/DNA Repair
SIRT6-IN-3 (compound 8a) 作为SIRT6的选择性抑制剂,其IC50值为7.49 μM。该化合物能有效抑制胰腺导管腺癌 (PDAC) 细胞的增殖,并诱导细胞凋亡。SIRT6-IN-3 通过抑制 DNA 损伤的修复作用,增强了吉西他滨对癌细胞的敏感性,常用于胰腺癌相关研究。
T79647 VEGFR/PARP-IN-1

PARP Chromatin/Epigenetic; DNA Damage/DNA Repair
VEGFR/PARP-IN-1 (Compound 14b) 是一款针对VEGFR和PARP两个靶点的双重抑制剂,其对VEGFR和PARP的IC50值分别为191 nM和60.9 nM。该化合物能够抑制DNA损伤修复机制,诱导apoptosis,并使细胞在G2/M期阻滞。此外,VEGFR/PARP-IN-1对BRCA野生型乳腺癌细胞表现出较强的抗增殖效果,尤其是在MDA-MB-231和MCF-7细胞系上,其IC50值分别为4.1 μM和3.5 μM,是潜在的抗肿瘤和抗转移药物。
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。
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)。

化合物

GeA-69
Cat.No: T5399
Synonym:
Target: PARP
Elimusertib
Cat.No: T7318
Synonym: BAY-1895344
Target: ATM/ATR
DDRI-18
Cat.No: T23974
Synonym: DDRI18,DDRI 18
Target: DNA/RNA Synthesis
Emzadirib
Cat.No: T12682
Synonym: CYT-0851,RAD51-IN-2
Target: DNA/RNA Synthesis
Tuvusertib
Cat.No: T10406
Synonym: M1774,ATR inhibitor 1
Target: Apoptosis, ATM/ATR, Others, Chk
Niraparib
Cat.No: T3231
Synonym: 尼拉帕尼,MK-4827
Target: Apoptosis, Others, PARP
TIQ-A
Cat.No: T50098
Synonym:
Target: PARP
M3541
Cat.No: T70873
Synonym:
Target: Apoptosis, ATM/ATR
Methoxyamine HCl
Cat.No: T21320
Synonym: 甲氧基胺盐酸盐,TRC102,TRC 102,Methoxyamine,TRC-102
Target: Others
MS0017509
Cat.No: T25838
Synonym: MS-0017509,MS 0017509
Target:
MS0019266
Cat.No: T25839
Synonym: MS 0019266,MS-0019266
Target:
MFH290
Cat.No: T69931
Synonym:
Target:
AV-153
Cat.No: T40345
Synonym:
Target:
Tetrapeptide
Cat.No: T80207
Synonym:
Target: DNA/RNA Synthesis
SNM1A-IN-1
Cat.No: T81140
Synonym:
Target:
ATR-IN-5
Cat.No: T63923
Synonym:
Target:
Phosphoramide mustard (cyclohexanamine)
Cat.No: T36701
Synonym:
Target:
Amuvatinib hydrochloride
Cat.No: T14282
Synonym: HPK 56 hydrochloride,MP470 hydrochloride
Target: Others
Ceralasertib formate
Cat.No: T26981
Synonym: Ceralasertib,AZD-6738,AZD 6738,AZD6738
Target:
Selenocystine
Cat.No: T78581
Synonym:
Target: Others
FEN1-IN-2
Cat.No: T40931
Synonym:
Target: Others
Iproplatin
Cat.No: T32189
Synonym: JM-9,CHIP,Code name: JM9,JM 9
Target:
Ru3
Cat.No: T81249
Synonym:
Target: PARP
Ethylenediaminetetraacetic acid dipotassium dihydrate
Cat.No: T75335
Synonym:
Target:
NSC15520
Cat.No: T81640
Synonym:
Target:
SZUH280
Cat.No: T75021
Synonym:
Target:
5-Hydroxy Lansoprazole Sulfide
Cat.No: T70978
Synonym:
Target:
IMP-1700
Cat.No: T37729
Synonym:
Target:
APE1-IN-2
Cat.No: T73299
Synonym:
Target: Apoptosis
AV-153 free base
Cat.No: T60649
Synonym:
Target:
FEN1-IN-6
Cat.No: T79134
Synonym:
Target: FLAP
ATR-IN-6
Cat.No: T63555
Synonym:
Target:
FEN1-IN-7
Cat.No: T79135
Synonym:
Target: FLAP
PARP-1/2-IN-2
Cat.No: T78787
Synonym:
Target: PARP
SIC5-6
Cat.No: T78138
Synonym:
Target: Others
SIRT6-IN-3
Cat.No: T79689
Synonym:
Target: Sirtuin
VEGFR/PARP-IN-1
Cat.No: T79647
Synonym:
Target: PARP
BRC4wt TFA
Cat.No: T83854
Synonym:
Target:
PARP1/BRD4-IN-2
Cat.No: T62540
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T4971 5'-DEOXYADENOSINE

5′-dAdo,5-脱氧腺嘌呤核苷

Endogenous Metabolite Metabolism
5'-Deoxyadenosine (5′-dAdo) 是正常受试者尿液中发现的氧化核苷,氧化核苷代表了用于确定遗传物质损伤程度的生物标志物。
T10018 1-Methyladenine

Others Others
1-Methyladenine is a DNA alkylation product that undergoes damage reversal through oxidative demethylation for repair purposes.

天然产物

5'-DEOXYADENOSINE
Cat.No: T4971
Synonym: 5′-dAdo,5-脱氧腺嘌呤核苷
Target: Endogenous Metabolite
1-Methyladenine
Cat.No: T10018
Synonym:
Target: Others
TargetMol Loading
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