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37

抑制剂 & 化合物

3

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T12019	Methylproamine	Others	Others
	Methylproamine 是一种与DNA 结合的辐射保护剂，可以修复辐射诱导的短暂活性氧。
T6878	LJI308	S6 Kinase	MAPK; PI3K/Akt/mTOR signaling
	LJI308 是泛RSK 抑制剂，对 RSK1、RSK2 和 RSK3 的IC50分别为 6、4 和 13 nM。它抑制辐照、EGF 处理和表达 KRAS 突变的细胞中 RSK (T359/S363) 和 YB-1 (S102) 的磷酸化。
T9168	NSC 617145 NSC617145,NSC-617145	DNA/RNA Synthesis	Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	NSC 617145 (NSC617145) 是一种 WRN 解旋酶抑制剂，IC50值为 230 nM。它以浓度依赖性方式抑制 WRN 解旋酶的 ATP 酶，并诱导双链断裂和染色体异常。
T24925	UNC-2170 UNC2170 Maleate,UNC-2170 Maleate,UNC 2170 Maleate	Others	Others
	UNC-2170 (UNC2170 Maleate) 是53BP1(IC50=29 µM;Kd=22 µM) 选择性的、功能活性的片段状配体，对 53BP1 的选择性比其他九种甲基赖氨酸读取器蛋白质高出至少17倍。53BP1 是 Kme 结合蛋白，在 DNA 损伤修复途径中起核心作用，并被招募到双链断裂位点。
T14858	Calicheamicin Calicheamicin γ1,卡奇霉素	Others	Others
	Calicheamicin (Calicheamicin γ1) 是肿瘤抗生素，可引起DNA 双链断裂，抑制DNA 合成。
T8880	PFM01	Others	Others
	PFM01 是 MRE11核酸内切酶抑制剂，是 N-烷基化的 Mirin 衍生物。它可以通过非同源末端连接 (NHEJ) 和同源重组 (HR) 调节双链断裂修复 (DSBR)。
T11600	IBR2 Isoquinoline	DNA/RNA Synthesis	Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	IBR2（Isoquinoline）是一种针对RAD51的强效特异性抑制剂，通过干预RAD51多聚体形成，加速蛋白酶体介导的RAD51蛋白降解，抑制癌细胞生长并诱导凋亡。实验证明在抑制RAD51介导的DNA双链断裂修复方面有效。
T63228	Simmiparib SMOCL-9112	Apoptosis; PARP	Apoptosis; Chromatin/Epigenetic; DNA Damage/DNA Repair
	Simmiparib (SMOCL-9112) 是一种新型有效的 PARP1 和 PARP2 抑制剂，是一种Olaparib 衍生物。Simmiparib 在同源重组修复 (HR) 缺陷细胞中诱导 DNA 双链断裂 (DSB) 和细胞周期阻滞，从而促使细胞凋亡 (apoptosis)。Simmiparib 可用于研究帕金森病、阿尔茨海默病、乳腺癌和黑色素瘤。
T9760	IC 86621	DNA-PK	DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling
	IC 86621 是一种选择性和可逆的 ATP 竞争性 DNA-PK 抑制剂，IC50 为 120 nM。 IC 86621 增加 DNA 双链断裂 (DSB) 诱导的抗肿瘤活性，其 EC50 为 68 µM，用于 DNA-PK 介导的细胞 DSB 修复。
T11067	VX-984 M9831	DNA-PK	DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling
	VX-984 (M9831) 是一种可口服的、具有选择性的的、可透过血脑屏障的 DNA-PK 抑制剂。VX-984 对非同源性末端 NHEJ 的接合具有抑制作用，可作用于 DSBs 使 DNA 双链断裂。VX-984常见于对胶质母细胞瘤 (GBM) 和非小细胞肺癌 (NSC-LC) 的研究。
T3157	COH29 RNR Inhibitor COH29	DNA/RNA Synthesis	Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	COH29 (RNR Inhibitor COH29) 是一种口服可用的芳香族取代噻唑，是人类核糖核苷酸还原酶 (RNR) 的抑制剂，具有潜在的抗肿瘤活性。它抑制核糖核苷酸还原酶的IC50为 16 μM。
T71825	BEPP monohydrochloride
	BEPP monohydrochloride is a double-strand RNA-dependent protein kinase (PKR) activator.
T21303	Etoposide Phosphate Eposin Etopophos Vepesid VP16,磷酸依托泊苷
	Etoposide phosphate is a phosphate salt of Etoposide, which binds to the enzyme topoisomerase II, then induces double-strand DNA breaks and inhibits DNA repair, leading to decreased DNA synthesis and tumor cell proliferation.
T16283	Neocarzinostatin	5-HT Receptor	GPCR/G Protein; Neuroscience
	Neocarzinostatin is an effective DNA-damaging, anti-tumor antibiotic. It recognizes double-stranded DNA bulge and induces DNA double strand breaks (DSBs). Neocarzinostatin leads to apoptosis. Neocarzinostatin has potential for EpCAM-positive cancer treatment.
T19149	5-BrdUTP sodium salt 5-Bromo-2'-deoxyuridine 5'-triphosphate sodium salt	Others	Others
	5-BrdUTP sodium salt is a TdT substrate that can be used to label the DNA double-strand breaks.
T68985	Amonafide L-malate
	Amonafide L-malate is the malate salt of amonafide, an imide derivative of naphthalic acid, with potential antineoplastic activity. Amonafide intercalates into DNA and inhibits topoisomerase II, resulting in DNA double-strand breaks (DSB) and inhibition of DNA replication and RNA synthesis.
T60621	PFM03
	PFM03 是MRE11 核酸内切酶抑制剂，可通过非同源末端连接 (NHEJ) 调节 DNA 双链断裂修复 (DSBR) [1]。
T68673	Amsacrine gluconate
	Amsacrine gluconate is an aminoacridine derivative with potential antineoplastic activity. Although its mechanism of action is incompletely defined, amsacrine may intercalate into DNA and inhibit topoisomerase II, resulting in DNA double-strand breaks, arrest of the S/G2 phase of the cell cycle, and cell death.
T68672	Amsacrine lactate
	Amsacrine lactate is an aminoacridine derivative with potential antineoplastic activity. Although its mechanism of action is incompletely defined, amsacrine may intercalate into DNA and inhibit topoisomerase II, resulting in DNA double-strand breaks, arrest of the S/G2 phase of the cell cycle, and cell death.
T68671	Amsacrine Isothionate
	Amsacrine Isothionate is an aminoacridine derivative with potential antineoplastic activity. Although its mechanism of action is incompletely defined, amsacrine may intercalate into DNA and inhibit topoisomerase II, resulting in DNA double-strand breaks, arrest of the S/G2 phase of the cell cycle, and cell death.
TD0003L	CelGreen nucleic acid gel stain 10,000× concentrate in DMSO
	CelGreen nucleic acid gel stain 10,000× concentrate in DMSO is a fluorescent dye with a unique involvement that binds to all dsDNA double helix sulcus regions.In the free state, the side strand and CelGreen emit weak fluorescence, but the fluorescence is greatly enhanced once they are combined with the double-stranded DNA. Therefore, the fluorescence signal strength of CelGreen is related to the amount of double-stranded DNA, and the amount of double-stranded DNA in the PCR system can be detec...
T76109	Nuclease S1
	Nuclease S1 是一种特异性的核酸内切酶，可降解单链 DNA (ssDNA) 和 RNA。Nuclease S1 还可以去除双链 DNA 中突出的单链末端。
T79330	PARP-1-IN-13	PARP	Chromatin/Epigenetic; DNA Damage/DNA Repair
	PARP-1-IN-13 (Compound 19c) 为一种高效PARP-1抑制剂，其IC50值为26 nM。该化合物能够抑制DNA单链断裂修复并增强DNA双链断裂效应。此外，PARP-1-IN-13通过激活线粒体凋亡(apoptosis)途径来促进癌细胞死亡。
T23654	Afeletecan free base BAY 56-3722,BAY56-3722,BAY-563722,Afeletecan
	Afeletecan is a water-soluble camptothecin derivative. Afeletecan stabilizes the topoisomerase I-DNA covalent complex and forms an enzyme-drug-DNA ternary complex. Both the initial cleavage reaction and religation steps are inhibited and subsequent collis
T61664	Benzoquinoquinoxaline
	Benzoquinoquinoxaline (BQQ) is a heterocyclic compound featuring an aminoalkyl side chain. BQQ exhibits preferential binding to DNA triplex structures, intercalating between the bases to stabilize the triplex conformation. Additionally, conjugation of BQQ to 1,10-phenanthroline enables specific binding and cleavage of double-strand DNA at the site where a triplex structure forms [1].
T69862	Afeletecan HCl
	Afeletecan, also known as BAY 56-3722, is a water-soluble camptothecin derivative conjugated to a carbohydrate moiety exhibiting antineoplastic activity. BAY 56-3722 stabilizes the topoisomerase I-DNA covalent complex and forms an enzyme-drug-DNA ternary complex. As a consequence of the formation of this complex, both the initial cleavage reaction and religation steps are inhibited and subsequent collision of the replication fork with the cleaved strand of DNA results in inhibition of DNA repli...
T78747	DiPT-4	Topoisomerase	DNA Damage/DNA Repair
	DiPT-4为一种TOP1/PARP1双重抑制剂，可引发癌细胞大量DNA双链断裂(DSB)、细胞周期阻滞及凋亡。DiPT-4具有研究癌症耐药性克服潜力。
T68870	SU-11752
	SU-11752 is a potent and selective DNA-PK inhibitor. Inhibition kinetics and a direct assay for ATP binding showed that SU11752 inhibited DNA-PK by competing with ATP. SU11752 inhibited DNA double-strand break repair in cells and gave rise to a five-fold sensitization to ionizing radiation. At concentrations of SU11752 that inhibited DNA repair, cell cycle progression was still normal and ATM kinase activity was not inhibited.
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。
TD0003	CelGreen nucleic acid gel stain 10,000× concentrate in water	Others	Others
	CelGreen 是一种具有独特参与性的荧光染料，可与所有 dsDNA 双螺旋沟区域结合。在游离状态下，侧链和 CelGreen 发出微弱的荧光，但一旦与双链DNA 结合，荧光就会大大增强。因此，CelGreen 的荧光信号强度与双链DNA 的量有关，可以根据荧光信号检测PCR 系统中双链DNA 的量。
T79925	T4 UvsX Recombinase	DNA/RNA Synthesis	Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	T4 UvsX Recombinase 促进双链DNA模板上DNA复制的启动，通过催化模板DNA与同源单链DNA引物间的突触形成。此酶显著增强了T4 DNA聚合酶全酶在线性单链DNA模板上进行的回跳（发夹引物）DNA合成反应。
T80899	UNC3474
	UNC3474为小分子配体，与53BP1相结合。该化合物针对53BP1TT的芳香族甲基赖氨酸结合笼展现出1.0 ± 0.3μM的解离常数（Kd）。UNC3474抑制53BP1募集至DSB，其机制为稳定细胞内预存的53BP1自抑制状态。
T73023	PARP1-IN-12
	PARP1-IN-12 是一种有效的PARP1抑制剂，其IC50值为 2.99 nM。PARP1-IN-12 具有较好的抗癌细胞增殖活性，可诱导细胞凋亡并使细胞周期停滞在 G2/M 期。PARP1-IN-12 能在BRCA 缺陷的细胞中诱导 DNA 双链断裂 (DSBs)。
T74501	NHEJ inhibitor-1
	NHEJ inhibitor-1 (Compound C2) 是一种三功能 Pt(II) 复合物，可缓解非同源末端连接 (NHEJ)/同源重组 (HR) 相关的双链断裂 (DSB) 修复，从而避免非小细胞肺对顺铂的耐药性。NHEJ inhibitor-1 抑制损伤修复蛋白 Ku70 和 Rad51，从而使肿瘤对活性分子重新敏感。NHEJ inhibitor-1 还诱导 ROS 产生和MMP 降低。
T79405	PARP1-IN-15	PARP	Chromatin/Epigenetic; DNA Damage/DNA Repair
	PARP1-IN-15（Compound 6）是一款针对PARP1的抑制剂，能够抑制坦聚合酶(TNKS)并促进DNA双链断裂损伤。该化合物在诱导肿瘤细胞凋亡(apoptosis)方面具有显著作用，且在三阴性乳腺癌(TNBC)细胞及来源于TNBC患者的类器官中显示出抗癌活性，适用于探究BRCA1突变状态下的TNBC研究。
T61017	Topoisomerase II inhibitor 6
	Topoisomerase II inhibitor 6 (Compound 5) 是色胺酮的衍生物。它是一种有效的拓扑异构酶的选择性抑制剂。Topoisomerase II inhibitor 6 在 G2 期阻断 CCRF-CEM 的细胞周期并诱导 DNA 双链断裂。Topoisomerase II inhibitor 6 对不同的肿瘤细胞系具有抗增殖活性，在癌症疾病研究中具有潜力。
T61369	p53 Activator 2
	p53 Activator 2 (compound 10ah) 插入DNA，导致显著的DNA双链断裂。该化合物通过增加p53、p-p53、CDK4、p21的表达，使细胞周期在G2/M期停滞，诱导细胞凋亡，并显著降低抗凋亡蛋白Bcl-2、Bcl-xL和cyclin B1的水平。此外，p53 Activator 2表现出对MGC-803细胞的抗增殖效果，其IC50为1.73 μM，且在MGC-803异种移植肿瘤模型中展示出有效的抗癌活性。

化合物

Cat.No: T12019

Target: Others

Cat.No: T6878

Target: S6 Kinase

Cat.No: T9168

Synonym: NSC617145,NSC-617145

Target: DNA/RNA Synthesis

Cat.No: T24925

Synonym: UNC2170 Maleate,UNC-2170 Maleate,UNC 2170 Maleate

Target: Others

Cat.No: T14858

Synonym: Calicheamicin γ1,卡奇霉素

Target: Others

Cat.No: T8880

Target: Others

Cat.No: T11600

Synonym: Isoquinoline

Target: DNA/RNA Synthesis

Cat.No: T63228

Synonym: SMOCL-9112

Target: Apoptosis, PARP

Cat.No: T9760

Target: DNA-PK

Cat.No: T11067

Synonym: M9831

Target: DNA-PK

Cat.No: T3157

Synonym: RNR Inhibitor COH29

Target: DNA/RNA Synthesis

BEPP monohydrochloride

Cat.No: T71825

Etoposide Phosphate

Cat.No: T21303

Synonym: Eposin Etopophos Vepesid VP16,磷酸依托泊苷

Neocarzinostatin

Cat.No: T16283

Target: 5-HT Receptor

5-BrdUTP sodium salt

Cat.No: T19149

Synonym: 5-Bromo-2'-deoxyuridine 5'-triphosphate sodium salt

Target: Others

Amonafide L-malate

Cat.No: T68985

Cat.No: T60621

Amsacrine gluconate

Cat.No: T68673

Amsacrine lactate

Cat.No: T68672

Amsacrine Isothionate

Cat.No: T68671

CelGreen nucleic acid gel stain *10,000× concentrate in DMSO*

Cat.No: TD0003L

Cat.No: T76109

Cat.No: T79330

Target: PARP

Afeletecan free base

Cat.No: T23654

Synonym: BAY 56-3722,BAY56-3722,BAY-563722,Afeletecan

Benzoquinoquinoxaline

Cat.No: T61664

Cat.No: T69862

Cat.No: T78747

Target: Topoisomerase

Cat.No: T68870

Cat.No: T78581

Target: Others

CelGreen nucleic acid gel stain *10,000× concentrate in water*

Cat.No: TD0003

Target: Others

T4 UvsX Recombinase

Cat.No: T79925

Target: DNA/RNA Synthesis

Cat.No: T80899

Cat.No: T73023

NHEJ inhibitor-1

Cat.No: T74501

Cat.No: T79405

Target: PARP

Topoisomerase II inhibitor 6

Cat.No: T61017

p53 Activator 2

Cat.No: T61369

Cat. No.	Product Name	Target	Signaling Pathways
TN1637	Eurycomalactone	Anti-infection; NF-κB	Microbiology/Virology; NF-κB
	Eurycomalactone 是一种NF-κB 抑制剂，IC50=0.5 μM，是一种天然产物。它可抑制蛋白合成，降低 cyclin D1 蛋白水平，但对 TNFα 诱导的 IκBα 降解或 IKKα/β 和 IκBα 的磷酸化水平没有作用。
T6228	Irinotecan CPT-11,Topotecin,伊立替康,(+)-Irinotecan	Topoisomerase; Autophagy	Autophagy; DNA Damage/DNA Repair
	Irinotecan (CPT-11) 是喜树碱的衍生物，是一种 DNA 拓扑异构酶 I (Topo I) 的抑制剂。Irinotecan 通过与 Topo I 复合物结合来阻止 DNA 链的重新连接，并导致双链 DNA 断裂和细胞死亡，具有抗肿瘤活性。
T35770	Cylindrospermopsin
	Cylindrospermopsin, a tricyclic uracil derivative, is a cyanobacterial toxin that was first discovered in an algal bloom contaminating a local drinking supply on Palm Island in Queensland, Australia after an outbreak of a mysterious disease. Cylindrospermopsin targets protein and glutathione synthesis in hepatocytes (IC50s = 1.3 and 2.4 &#181M, respectively), leading to cell death. [1] It has been shown to inhibit the activity of the uridine monophosphate synthase complex with a Ki value of 10 &...

天然产物

Eurycomalactone

Cat.No: TN1637

Target: Anti-infection, NF-κB

Cat.No: T6228

Synonym: CPT-11,Topotecin,伊立替康,(+)-Irinotecan

Target: Topoisomerase, Autophagy

Cylindrospermopsin

Cat.No: T35770

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