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DNA Damage

DNA Damage

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NSC-207895 (XI-006)

Catalog No. A11179
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MDMX 抑制剂

NSC-207895 (XI-006)是细胞可渗透的苯并呋喃化合物，可通过抑制MDMX启动子转录活性（IC50 = 2.5 ?M，下调MCF-7，LNCaP和A549细胞中的p53负调节剂MDMX蛋白水平（1至10 ?M，持续16至24 h）），导致增强的p53稳定和激活。了解更多

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Floxuridine

Catalog No. A10392
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DNA/RNA Synthesis 抑制剂

Floxuridine是一种抗肿瘤药，属于抗代谢物，是一种MDCK/PEPT1抑制剂。了解更多

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Mupirocin

Catalog No. A14230
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isoleucyl t-RNA synthetase 抑制剂

Mupirocin是一种异亮氨酰t-RNA合成酶抑制剂。了解更多

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Chloroambucil

Catalog No. A14252
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DNA/RNA Synthesis 抑制剂

Chloroambucil是氮芥芥烷化剂。了解更多

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Puromycin 2HCl

Catalog No. A14268
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protein synthesis 抑制剂

Puromycin 2HCl是一种氨基核苷抗生素，可作为蛋白质合成抑制剂。了解更多

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4E1RCat

Catalog No. A14301
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eIF4F subunit interaction 抑制剂

4E1RCat是eIF4E：eIF4G和eIF4E：4E-BP1相互作用的双重抑制剂。了解更多

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CRT0044876

Catalog No. A14304
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APE1 抑制剂

CRT0044876是一种有效的选择性APE1抑制剂，IC50约为3μM。了解更多

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4EGI-1

Catalog No. A14199
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eIF4E/eIF4G 抑制剂

4EGI-1是一种竞争性eIF4E/eIF4G相互作用抑制剂，KD值 25 uM。了解更多

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SCR7

Catalog No. A15447
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DNA ligase IV 抑制剂

SCR7是一种特定的DNA Ligase IV抑制剂。SCR7通过激活p53介导的细胞凋亡来抑制多种细胞类型中双链断裂的末端连接，从而导致肿瘤消退。了解更多

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Mitomycin C

Catalog No. A11491
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DNA synthesis 抑制剂

Mitomycin C是一种DNA交联剂，可抑制DNA合成并诱导多种细胞凋亡。了解更多

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L189

Catalog No. A15790
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DNA Ligase 抑制剂

L189是新型人类DNA连接酶抑制剂，可抑制hLigI/III/IV，IC50为5/9/5μM。了解更多

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E3330

Catalog No. A14440
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APE1 Redox 抑制剂

E3330是有效的选择性APE1（Ref-1）抑制剂，可抑制NF-κBDNA结合活性。了解更多

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6-Mercaptopurine Monohydrate

Catalog No. A15898
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de novo purine synthesis 抑制剂

6-Mercaptopurine Monohydrate是一种广泛使用的抗白血病药物和免疫抑制药物，通过将硫嘌呤甲基转移酶代谢物掺入DNA和RNA来抑制嘌呤从头合成。了解更多

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L67

Catalog No. A15978
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DNA ligases 抑制剂

L67是DNA连接酶抑制剂。L67抑制DNA连接酶I和III。L67是关于刻痕DNA的简单竞争性抑制剂。了解更多

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AN2718

Catalog No. A16203
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RNA synthetase 抑制剂

AN2718是一种新型的含硼小分子，可抑制必需的蛋白质合成酶，亮氨酰转移RNA合成酶或LeuRS。了解更多

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MB-7133

Catalog No. A22007
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DNA synthesis inhibitor

MB-7133 is a DNA synthesis inhibitor. 了解更多

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Fluorouracil (Adrucil)

Catalog No. A10042
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DNA and RNA synthesis 抑制剂

Fluorouracil (Adrucil)是一种是DNA/RNA合成抑制剂，通过不可逆地抑制胸苷酸合酶起作用。了解更多

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- T Hoshiba ,etc. Decellularized matrices as in vitro models of extracellular matrix in tumor tissues at different malignant levels: Mechanism of 5-fluorouracil resistance in colorectal tumor cells. Biochimica et Biophysica Acta (BBA)-Molecular Cell Research, 2016, 1863(11), 2749-2757.
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Cidofovir (Vistide)

Catalog No. A10214
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DNA/RNA Synthesis 抑制剂

Cidofovir (Vistide)通过选择性抑制病毒DNA的合成而抑制病毒复制。了解更多

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- Adhikary A, .et al. π-Radical to σ-Radical Tautomerization in One-Electron-Oxidized 1-Methylcytosine and Its Analogs, J Phys Chem B, 2015, Sep 3;119(35):11496-505 PMID: 26237072
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Clofarabine

Catalog No. A10228
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DNA/RNA Synthesis 抑制剂

Clofarabine具有抗肿瘤活性的第二代嘌呤核苷类似物。了解更多

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- Xie J, .et al. Optimization of a clofarabine-based drug combination regimen for the preclinical evaluation of pediatric acute lymphoblastic leukemia, Pediatr Blood Cancer, 2019, Dec 25:e28133 PMID: 31876116
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Cycloheximide (Actidione)

Catalog No. A10036
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Protein Synthesis 抑制剂

Cycloheximide (Actidione)用作选择性抗生素。它抑制腐菌真菌真核生物的蛋白质合成(DNA依赖性RNA)。通过与80S核糖体结合而对皮肤真菌和系统性真菌无效。了解更多

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- Ke Chen, .et al. Junction plakoglobin regulates and destabilizes HIF2α to inhibit tumorigenesis of renal cell carcinoma, Cancer Commun (Lond), 2021, Apr; 41(4): 316-332 PMID: 33591636
- Zhiyuan Qin, .et al. miR-224-5p Contained in Urinary Extracellular Vesicles Regulates PD-L1 Expression by Inhibiting Cyclin D1 in Renal Cell Carcinoma Cells, Cancers (Basel), 2021, Feb 4;13(4):618 PMID: 33557163
- Hua Xu, .et al. Preclinical Study Using ABT263 to Increase Enzalutamide Sensitivity to Suppress Prostate Cancer Progression Via Targeting BCL2/ROS/USP26 Axis Through Altering ARv7 Protein Degradation, Cancers (Basel), 2020, Apr; 12(4): 831 PMID: 32235588
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Gemcitabine HCl (Gemzar)

Catalog No. A10423
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DNA/RNA Synthesis 抑制剂

Gemcitabine HCl (Gemzar)是一种DNA synthesis抑制剂，作用于PANC1，MIAPaCa2，BxPC3和Capan2细胞，通过在癌细胞dna复制过程中取代核酸的一个组成部分，防止肿瘤生长。了解更多

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- G. R. Iglesias, .et al. Hyperthermia-Triggered Gemcitabine Release from Polymer-Coated Magnetite Nanoparticles, Polymers, 2018, 10(3), 269
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Bleomycin sulfate

Catalog No. A10152
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DNA/RNA Synthesis 抑制剂

Bleomycin Sulfate硫酸博来霉素是一种糖肽类抗生素，也是一种鳞状细胞癌(SCC)抗癌剂。了解更多

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- Mai Kanemaru, .et al. Nanoparticle-mediated local delivery of pioglitazone attenuates bleomycin-induced skin fibrosis, J Dermatol Sci, 2018, Jan;93(1):41-49 PMID: 30655107
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RK-33

Catalog No. A16194
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DDX3 抑制剂

RK-33是有效的选择性DDX3抑制剂。RK-33与DDX3结合并取消其活性。了解更多

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- Yang SNY, .et al. RK-33 Is a Broad-Spectrum Antiviral Agent That Targets DEAD-Box RNA Helicase DDX3X, Cells, 2020, Jan 9;9(1). PMID: 31936642
- Zhang S, .et al. Nuclear bodies formed by polyQ-ataxin-1 protein are liquid RNA/protein droplets with tunable dynamics, Sci Rep, 2020, Jan 31;10(1):1557 PMID: 32005838
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Tegafur

Catalog No. A10407
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DNA/RNA Synthesis 抑制剂

Tegafur是一种用于治疗癌症的化疗药物5-FU前药，是替加氟尿嘧啶的一种成分。了解更多

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- Takashi Azuma, .et al. Removal of pharmaceuticals in water by introduction of ozonated microbubbles, SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Azuma T, .et al. Distribution of six anticancer drugs and a variety of other pharmaceuticals, and their sorption onto sediments, in an urban Japanese river, Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. Detection of pharmaceuticals and phytochemicals together with their metabolites in hospital effluents in Japan, and their contribution to sewage treatment plant influents, Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
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YK 4-279

Catalog No. A11612
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RHA 抑制剂

YK 4-279是与致癌转录因子EWS-FLI1结合的RNA解旋酶A（RHA）抑制剂。了解更多

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- Christopher M Schafer, .et al. An inhibitor of endothelial ETS transcription factors promotes physiologic and therapeutic vessel regression, Proc Natl Acad Sci U S A, 2020, Oct 20;117(42):26494-26502 PMID: 33020273
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Daptomycin

Catalog No. A10289
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DNA/RNA Synthesis 抑制剂

Daptomycin是一种脂肽抗生素，用于治疗由革兰氏阳性生物体引起的某些感染。了解更多

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- Viktoria Lazar, .et al. Antibiotic combinations reduce Staphylococcus aureus clearance, Nature, 2022, 610: 540-546 PMID: 36198788
- Shigeru Fujimura, .et al. Antimicrobial efficacy of combined clarithromycin plus daptomycin against biofilms-formed methicillin-resistant Staphylococcus aureus on titanium medical devices., J Infect Chemother., 2015, Oct;21(10):756-9 PMID: 26162777
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Oxaliplatin (Eloxatin)

Catalog No. A10346
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DNA/RNA Synthesis 抑制剂

Oxaliplatin (Eloxatin)是一种DNA/RNA Synthesis抑制剂，具有抗结肠癌的抗肿瘤活性。了解更多

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- Mohamed Elbadawy, .et al. Anti-cancer activity of amorphous curcumin preparation in patient-derived colorectal cancer organoids, Biomed Pharmacother, 2021, Oct;142:112043 PMID: 34411919
- Tatsuya Usui, .et al. Hedgehog Signals Mediate Anti-Cancer Drug Resistance in Three-Dimensional Primary Colorectal Cancer Organoid Culture, Int J Mol Sci, 2018, Apr; 19(4): 1098 PMID: 29642386
- Shimokawa M, .et al. Visualization and targeting of LGR5+ human colon cancer stem cells, Nature, 2017, May 11;545(7653):187-192 PMID: 28355176
- Eri Takiguchi, .et al. Growth inhibitory effect of the Src inhibitor dasatinib in combination with anticancer agents on uterine cervical adenocarcinoma cells, Exp Ther Med, 2017, Nov; 14(5): 4293-4299 PMID: 29067110
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CX-5461

Catalog No. A11065
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DNA/RNA Synthesis 抑制剂

CX-5461是RNA聚合酶I（Pol I）的一流的非遗传毒性小分子靶向抑制剂，可激活p53途径而不会引起DNA损伤。了解更多

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- Taro Mannena, .et al. Distinct RNA polymerase transcripts direct the assembly of phase-separated DBC1 nuclear bodies in different cell lines, Mol Biol Cell, 2021, 32:ar33, 1?C11 PMID: 34495685
- Shuichiro Okamoto, .et al. The rRNA synthesis inhibitor CX-5461 may induce autophagy that inhibits anticancer drug-induced cell damage to leukemia cells, Biosci Biotechnol Biochem, 2020, Aug 15;1-8 PMID: 32799625
- Ahmed Abdullah Ahmed, .et al. A G-quadruplex-binding compound shows potent activity in human gemcitabine-resistant pancreatic cancer cells, Sci Rep, 2020, 10: 12192 PMID: 32699225
- Abed Saady, .et al. Applying styryl quinolinium fluorescent probes for imaging of ribosomal RNA in living cells, Dyes Pigm, 2020, 174: 107986
- Jackobel AJ, .et al. DNA binding preferences of S. cerevisiae RNA polymerase I Core Factor reveal a preference for the GC-minor groove and a conserved binding mechanism, Biochim Biophys Acta Gene Regul Mech, 2019, Aug 2:194408 PMID: 31382053
- Hiroaki Suzuki, .et al. The proline-arginine repeat protein linked to C9-ALS/FTD causes neuronal toxicity by inhibiting the DEAD-box RNA helicase-mediated ribosome biogenesi, Cell Death Dis, 2018, Oct; 9(10): 975 PMID: 30250194
- Anastasia Gelgor, .et al. Nucleolar stress enhances lytic reactivation of the Kaposi??s sarcoma-associated herpesvirus, Oncotarget, 2018, Mar 2; 9(17): 13822-13833 PMID: 29568397
- Wang ZF, .et al. The Hairpin Form of r(G4C2)exp in c9ALS/FTD Is Repeat-Associated Non-ATG Translated and a Target for Bioactive Small Molecules, Cell Chem Biol, 2018, Nov 29. pii: S2451-9456(18)30378-7 PMID: 30503283
- Yuko Fujiwara, .et al. A Nucleolar Stress-Specific p53-miR-101 Molecular Circuit Functions as an Intrinsic Tumor-Suppressor Network, EBioMedicine, 2018, Jul; 33: 33-48 PMID: 30049386
- Maïmouna Coura Kone, .et al. Three-Dimensional Distribution of UBF and Nopp140 in Relationship to Ribosomal DNA Transcription During Mouse Preimplantation Development, Biol Reprod, 2016, Apr;94(4):95, 1-12 PMID: 26984997
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AZ32

Catalog No. A16814
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ATM 抑制剂

AZ32是ATM激酶的特异性抑制剂，对小鼠具有良好的BBB渗透性，ATM酶的IC50值<0.0062 uM。它对ATR有足够的选择性，并且具有较高的细胞通透性。了解更多

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AZ31

Catalog No. A16813
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ATM 抑制剂

AZ31是一种新的选择性ATM抑制剂，IC50<0.0012 uM，对密切相关的酶具有良好的选择性（对DNA-PK和PI3Kα的选择性大于500倍，对mTOR、PI3Kβ和PI3Kγ的选择性大于1000倍）。了解更多

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AZD1390

Catalog No. A16798
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ATM 抑制剂

AZD1390是一流的口服中枢神经渗透性ATM抑制剂，在细胞中的IC50为0.78 nM，对PIKK酶家族中密切相关的成员具有10,000倍以上的选择性，并且在多种激酶中均具有出色的选择性。了解更多

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KU 59403

Catalog No. A20928
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ATM inhibitor

KU 59403 is a potent ATM inhibitor, with an IC50 of 3 nM. 了解更多

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CP-466722

Catalog No. A11086
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ATM 抑制剂

CP-466722是一种特殊的ATM抑制剂，可抑制细胞依赖ATM的磷酸化事件，并且ATM功能的破坏会导致特征性的细胞周期检查点缺陷。了解更多

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Torin 2

Catalog No. A11586
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mTOR 抑制剂

Torin 2 是有效的选择性mTOR抑制剂 (IC50 = 2.1 nM)。在PI3K上显示mTOR的800倍细胞选择性（mTOR和PI3K的细胞EC50值分别为0.25和200 nM）。了解更多

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- Diane Yang, .et al. Pancreatic Differentiation of Stem Cells Reveals Pathogenesis of a Syndrome of Ketosis-Prone Diabetes, Diabetes, 2021, Oct;70(10):2419-2429 PMID: 34344789
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CGK 733

Catalog No. A13191
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ATM/ATR 抑制剂

CGK733是ATR和ATM激酶的选择性抑制剂。在过早衰老的乳腺癌细胞中诱导细胞死亡。了解更多

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AZ-20

Catalog No. A13205
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ATR kinase 抑制剂

AZ20是一种有效的选择性ATR抑制剂，IC50值为5 nM。了解更多

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VE-822

Catalog No. A13289
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ATR 抑制剂

VE-822是有效的ATR抑制剂。了解更多

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Mirin

Catalog No. A15842
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ATM 抑制剂

Mirin可防止ATM激活以响应双链断裂（IC50 = 12 uM），并诱导G2细胞周期停滞。了解更多

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Wortmannin

Catalog No. A11161
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PI3K 抑制剂

Wortmannin是一种有效的，选择性的，可透过细胞的且不可逆的磷脂酰肌醇3-激酶（PI 3-激酶）（IC50 = 2-4 nM）抑制剂，它也有效抑制polo-like激酶1（PLK1）（IC50 = 5.8 nM）。了解更多

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- Dongdong Fang, etc. Epithelial-Mesenchymal Transition of Ovarian Cancer Cells Is Sustained by Rac1 through Simultaneous Activation of MEK1/2 and Src Signaling Pathways. Oncogene. 2017 Mar; 36(11): 1546–1558.
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AZD6738 (Ceralasertib)

Catalog No. A15794
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ATR 抑制剂

AZD6738是一种有效的ATR激酶抑制剂，对分离的酶的IC50为1 nM，对细胞中ATR激酶依赖性CHK1磷酸化的IC50为74 nM。了解更多

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- Brian F Kiesel, .et al. Dose-dependent bioavailability and tissue distribution of the ATR inhibitor AZD6738 (ceralasertib) in mice, Cancer Chemother Pharmacol, 2022, Feb;89(2):231-242 PMID: 35066692
- Albert Job, .et al. The POLD1 R689W variant increases the sensitivity of colorectal cancer cells to ATR and CHK1 inhibitors, Sci Rep, 2020, Nov 3;10(1):18924 PMID: 33144657
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AZD0156

Catalog No. A16419
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ATM 抑制剂

AZD0156是有效且选择性的ATM激酶抑制剂，具有潜在的化学/放射致敏和抗肿瘤活性。了解更多

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- Yi-Ru Pan, .et al. ATM Inhibitor Suppresses Gemcitabine-Resistant BTC Growth in a Polymerase θ Deficiency-Dependent Manner, Biomolecules, 2020, Nov 9;10(11):1529 PMID: 33182492
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VE-821

Catalog No. A11605
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ATM/ATR 抑制剂

VE-821是一种有效且选择性的蛋白激酶ATR抑制剂。了解更多

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- Mitsuru Sasaki-Honda, .et al. A patient-derived iPSC model revealed oxidative stress increases facioscapulohumeral muscular dystrophy-causative DUX4, Hum Mol Genet, 2018, Dec 1; 27(23): 4024-4035 PMID: 30107443
- Kim J, .et al. Replication Stress Shapes a Protective Chromatin Environment across Fragile Genomic Regions, Mol Cell, 2018, Jan 4;69(1):36-47.e7 PMID: 29249653
- Antonio Postigo, .et al. Cytoplasmic ATR Activation Promotes Vaccinia Virus Genome Replication, Cell Rep, 2017, May 2; 19(5): 1022-1032 PMID: 28467896
- Nnennaya Kanu, .et al. DNA replication stress mediates APOBEC3 family mutagenesis in breast cancer, Genome Biol, 2016, 17: 185 PMID: 27634334
- Carolyn Botting, .et al. H2AX phosphorylation and DNA damage kinase activity are dispensable for herpes simplex virus replication, Virol J, 2016, 13: 15 PMID: 26817608
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KU-55933

Catalog No. A10506
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ATM 抑制剂

KU-55933是ATM抑制剂，通过抑制细胞增殖，并通过阻断Akt过度激活的癌细胞中的Akt诱导凋亡。了解更多

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- Mariko Shikata, .et al. 4-(Methylnitrosamino)-1-(3-pyridyl)-1-butanone-Induced Histone Acetylation via α7nAChR-Mediated PI3K/Akt Activation and Its Impact on γ-H2AX Generation, Chem Res Toxicol, 2021, Dec 20;34(12):2512-2521 PMID: 34784199
- Masaya Igase, .et al. Combination Therapy with Reovirus and ATM Inhibitor Enhances Cell Death and Virus Replication in Canine Melanoma, Mol Ther Oncolytics, 2019, vol 15 PMID: 31650025
- Hayakawa K, .et al. Planar compression of extracellular substrates induces S phase arrest via ATM-independent CHK2 activation, Biochem Biophys Res Commun, 2018, Dec 2;506(4):983-989 PMID: 30404732
- Chwastek J, .et al. The ATM kinase inhibitor KU-55933 provides neuroprotection against hydrogen peroxide-induced cell damage via a γH2AX/p-p53/caspase-3-independent mechanism: Inhibition of calpain and cathepsin D, Int J Biochem Cell Biol, 2017, Jun;87:38-53 PMID: 28341201
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KU-60019

Catalog No. A10507
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ATM 抑制剂

KU-60019是一种强效特异性ATM抑制剂，IC50为6.3 nM。了解更多

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- Fu-Xing Gong, .et al. De-dimerization of PTB is catalyzed by PDI and is involved in the regulation of p53 translation, Nucleic Acids Res, 2021, Sep 20;49(16):9342-9352 PMID: 34403458
- Hegedus C, .et al. PARP1 Inhibition Augments UVB-Mediated Mitochondrial Changes-Implications for UV-Induced DNA Repair and Photocarcinogenesis, Cancers (Basel), 2019, Dec 18;12(1) PMID: 31861350
- Masaya Igase, .et al. Combination Therapy with Reovirus and ATM Inhibitor Enhances Cell Death and Virus Replication in Canine Melanoma, Mol Ther Oncolytics, 2019, vol 15 PMID: 31650025
- CHENGHUA LOU, .et al. Targeting the ataxia telangiectasia mutated pathway for effective therapy against hirsutine-resistant breast cancer cells, Oncol Lett, 2016, Jul; 12(1): 295-300 PMID: 27347141
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BEZ235 (NVP-BEZ235, Dactolisib)

Catalog No. A10133
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PI3K/mTOR 抑制剂

BEZ235 (NVP-BEZ235,Dactolisib)是通过与这些酶的ATP结合裂隙结合来抑制PI3K和mTOR激酶活性。了解更多

Product Citations (3)

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- Makoto Koyama, .et al. Low-dose trametinib and Bcl-xL antagonist have a specific antitumor effect in KRAS-mutated colorectal cancer cells, Int J Oncol, 2020, Sep 2 PMID: 32901840
- Tzeng SF, .et al. O-Glycosylation-mediated signaling circuit drives metastatic castration-resistant prostate cancer, FASEB J, 2018, Jun 15:fj201800687 PMID: 29906246
- Dominik Schulz, .et al. HNSCC cells resistant to EGFR pathway inhibitors are hypermutated and sensitive to DNA damaging substances, Am J Cancer Res, 2016, 6(9): 1963-1975 PMID: 27725902
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Costunolide

Catalog No. A10240
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Telomerase 抑制剂

Costunolide是人类端粒酶活性的抑制剂（MCF-7乳腺癌细胞中IC50 = 65μM）。了解更多

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RHPS4

Catalog No. A16354
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Telomerase 抑制剂

RHPS4是亚微摩尔浓度下端粒酶的有效抑制剂。了解更多

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BIBR 1532

Catalog No. A10140
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Telomerase 抑制剂

BIBR 1532是一种选择性端粒酶抑制剂（人端粒酶，人RNA聚合酶I和人RNA聚合酶II + III的IC50值分别为93，> 100000和> 100000 nM）。了解更多

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- Hosoi T, .et al. Inhibition of telomerase causes vulnerability to endoplasmic reticulum stress-induced neuronal cell death, Neurosci Lett, 2016, Aug 26;629:241-244 PMID: 27443785
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Norfloxacin (Norxacin)

Catalog No. A10652
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Topoisomerase 抑制剂

Norfloxacin(Norxacin)是一种广谱抗生素。了解更多

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Marbofloxacin

Catalog No. A10557
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Topoisomerase 抑制剂

Marbofloxacin是有效的第三代氟喹诺酮类抗生素，通过抑制细菌DNA复制起作用。了解更多

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溶液配制计算器

分子量计算器

稀释计算器

摩尔浓度计算器

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