39
2
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)。 |
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. |