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20

抑制剂 & 化合物

9

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T14349	Auristatin F	Microtubule Associated	Cytoskeletal Signaling
	Auristatin F 是一种有效的微管抑制剂和血管损伤剂。 Auristatin F 可用于抗体-药物偶联物。
T6116L	Bleomycin hydrochloride	DNA/RNA Synthesis	Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	Bleomycin hydrochloride is a potent antitumor antibiotic that functions as a DNA synthesis inhibitor and DNA damaging agent.
T2213	Terconazole Gyno-Terazol,Terazol 3,Terazol 7,Triaconazole,特康唑,曲康唑,R42470	Antifection; Antifungal	Microbiology/Virology
	Terconazole (Terazol 7) 是一种广谱抗真菌药物，用于研究阴道酵母菌感染。
T77520	AOH1996	Apoptosis; DNA/RNA Synthesis	Apoptosis; Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	AOH1996 是一种具有口服活性的复制体组分 PCNA (增殖细胞核抗原) 配体，靶向转录-复制冲突 (TRC)。AOH1996 可干扰 PCNA 与其结合蛋白的相互作用，导致 DNA 复制应激，诱导细胞凋亡 (apoptosis)。AOH1996 通过稳定 PCNA 和 RNA 聚合酶 II 的相互作用从而导致蛋白酶体依赖的 rpb1 降解和致命的 DNA 损伤。AOH1996 与 DNA 损伤剂具有协同作用，可抑制肿瘤细胞生长。
T41163	ZNL 02-096 Pomalidomide-C3-adavosertib	Apoptosis; Wee1	Apoptosis; Cell Cycle/Checkpoint
	ZNL 02-096 (Pomalidomide-C3-adavosertib) 是一种快速和选择性的 Wee1 降解剂 (IC50=3.58 nM)。ZNL 02-096 可在亚摩尔浓度下选择性降解 Wee1，而不损伤 AZD 1775 的二级靶点 PLK1。在体外 MOLT-4 细胞中，ZNL 02-096 可诱导 Wee1 降解、DNA 损伤积累、细胞周期停滞在 G2/M 期和细胞凋亡。ZNL 02-096 在 300 种癌症细胞系中显示出抗增殖作用。
T36733	HLI373 dihydrochloride
	HLI373 dihydrochloride is a potent Hdm2 inhibitor, efficiently restraining the ubiquitin ligase activity of Hdm2 and effectively prompting apoptosis in DNA-damaging agent-sensitive tumor cells[1]. Additionally, HLI373 dihydrochloride exhibits antimalarial activity[2].
T29263	(S,S)-D211 (S,S)-D-211,IQB dimer (S,S)-D211
	(S,S)-D211 is a DNA damaging payload.
T20788	Empenthrin MA-108,S2852,S 2852,MA108,S-2852,MA 108
	Empenthrin, a synthetic pyrethroid used in insecticides, is active against broad spectrum of flying insects including moths and other pests damaging textile.
T24176	(-)-Irofulven MGI-114,NSC-683863,MGI 114,HMAF,MGI114,Irofulven
	Irofulven is an agent of DNA-damaging and antitumor. It is used for the treatment of advanced solid tumors, including prostate, ovarian, and pancreatic cancers.
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.
T80132	CBP501 Affinity Peptide
	CBP501 Affinity Peptide为Chk激酶抑制剂，具有消除DNA损伤剂诱导的G2停滞作用，主要应用于癌症研究领域。
T38414	NSC 80467
	NSC 80467, a selective DNA damaging agent, functions by inhibiting survivin. Specifically, it preferentially targets DNA synthesis, leading to the induction of two distinct markers of DNA damage, namely γH2AX and pKAP1.
T37322	Steryl Glucosides
	Steryl glucosides are neutral glycolipids commonly found in plant cell membranes and vegetable oils that contain a glucose moiety conjugated to a sterol lipid. They function as glucose donors in the biosynthesis of glucocerebrosides in plant microsomes and are metabolic precursors to acylated/esterified steryl glucosides. Steryl glucosides are the major component of filter- and engine-damaging precipitates formed during biodiesel production from transesterification of vegetable oils. This produ...
T73719	Azoxymethane AOM	DNA	DNA Damage/DNA Repair
	Azoxymethane (AOM) 是一种 DNA 损伤剂，可诱导癌症生成，可用于制作结直肠癌小鼠模型。
T62683	PRMT5-IN-3
	PRMT5-IN-3 是一种 PRMT5 抑制剂。PRMT5-IN-3 联合 DNA 损伤剂，对肿瘤细胞具有合成致死性。
T78166	MEL24	Others	Others
	MEL24为Mdm2 E3连接酶抑制剂，通过p53依赖机制降低细胞存活率，增强对DNA损伤剂的敏感性，适用于体外抗肿瘤研究。
T22087	HLI 373
	HLI373 是一种有效的 Hdm2抑制剂, Hdm2 是一种泛素连接酶(E3)。HLI373 可有效诱导肿瘤细胞 (对 DNA 破坏剂敏感的) 凋亡 (apoptosis)，并且具有抗疟疾 (antimalarial) 活性。
T70115	Pamiparib hydrate
	Pamiparib, also known as BGB-290, is a highly potent and selective PARP inhibitor with favorable drug metabolism and pharmacokinetic properties. BGB-290 selectively binds to PARP and prevents PARP-mediated repair of single-strand DNA breaks via the base-excision repair (BER) pathway. This enhances the accumulation of DNA strand breaks, promotes genomic instability, and eventually leads to apoptosis. BGB-290 may both potentiate the cytotoxicity of DNA-damaging agents and reverse tumor cell chemo...
T77031	Ifabotuzumab
	Ifabotuzumab (KB004) 是靶向 EphA3的 IgG1κ 抗体 (KD=610 pM)。Ifabotuzumab 能够导致肿瘤细胞凋亡，并激活抗体依赖性细胞介导的细胞毒作用 (ADCC)，破坏肿瘤脉管系统。Ifabotuzumab 能够减少人特发性肺纤维化 (IPF) CCR10+细胞，改善肺纤维化。
T36673	CC 401 dihydrochloride
	High affinity JNK inhibitor (Ki values are 25-50 nM). Inhibits JNK via competitive binding of the ATP-binding site of active, phosphorylated JNK. Exhibits > 40-fold selectivity for JNK over p38, ERK, IKK2, protein kinase C, Lck and ZAP70. Hepatoprotective. Also inhibits HCMV replication. Uehara et al (2004) c-Jun N-terminal kinase mediates hepatic injury after rat liver transplantation. Transplantation. 78 324 PMID:15316358 \|Uehara et al (2005) JNK mediates hepatic ischemia reperfusion injury. J...

化合物

Cat.No: T14349

Target: Microtubule Associated

Bleomycin hydrochloride

Cat.No: T6116L

Target: DNA/RNA Synthesis

Cat.No: T2213

Synonym: Gyno-Terazol,Terazol 3,Terazol 7,Triaconazole,特康唑,曲康唑,R42470

Target: Antifection, Antifungal

Cat.No: T77520

Target: Apoptosis, DNA/RNA Synthesis

Cat.No: T41163

Synonym: Pomalidomide-C3-adavosertib

Target: Apoptosis, Wee1

HLI373 dihydrochloride

Cat.No: T36733

Cat.No: T29263

Synonym: (S,S)-D-211,IQB dimer (S,S)-D211

Cat.No: T20788

Synonym: MA-108,S2852,S 2852,MA108,S-2852,MA 108

Cat.No: T24176

Synonym: MGI-114,NSC-683863,MGI 114,HMAF,MGI114,Irofulven

Neocarzinostatin

Cat.No: T16283

Target: 5-HT Receptor

CBP501 Affinity Peptide

Cat.No: T80132

Cat.No: T38414

Steryl Glucosides

Cat.No: T37322

Cat.No: T73719

Synonym: AOM

Target: DNA

Cat.No: T62683

Cat.No: T78166

Target: Others

Cat.No: T22087

Pamiparib hydrate

Cat.No: T70115

Cat.No: T77031

CC 401 dihydrochloride

Cat.No: T36673

Cat. No.	Product Name	Target	Signaling Pathways
T5780	HYPOCRELLIN B	Apoptosis; Parasite; Antifungal	Apoptosis; Microbiology/Virology
	Hypocrellin B 是从真菌Hypocrella bambusae 和Shiraia bambusicola 中分离得到的一种感光颜料，可用于癌症光动力研究。它是一个凋亡诱导剂，还拥有抗菌和抗利什曼活性。
TMS2180	Zeaxanthin Anchovyxanthin,All-Trans-Zeaxanthin,玉米	Antioxidant; Endogenous Metabolite	Metabolism; oxidation-reduction
	Zeaxanthin (All-Trans-Zeaxanthin) 是食物获得类胡萝卜素，存在于眼睛的黄斑部，具有抗氧化活性。
T0146	Tioconazole UK-20349,Vagistat,噻康唑	Antibiotic; Antifection; Antifungal	Microbiology/Virology
	Tioconazole (Vagistat) 是一种广谱性的抗真菌咪唑衍生物。它抑制几种皮肤真菌和几种酵母菌的 MIC50分别小于 3.12 mg/L 和 9 mg/L。
T41245	Trimethylamine N-oxide	Reactive Oxygen Species; NOD-like Receptor (NLR); TGF-beta/Smad	Immunology/Inflammation; Metabolism; NF-κB; Stem Cells
	Trimethylamine N-oxide (TMAO）是由胆碱、甜菜碱和肉碱通过肠道微生物代谢产生的一种无色氧化胺，积聚在海洋动物的组织中，可预防尿素对蛋白质的破坏作用。Trimethylamine N-oxide 通过激活 ROS/NLRP3 炎性体诱导炎症，可诱导纤维细胞的分化和心脏纤维化。
T37876	Fengycin
	Fengycin is a cyclic lipopeptide used as an agricultural fungicide. Fengmycin has an anti-fungal infection effect by damaging the target’s cell membrane[1]. [1]. Sreyoshi Sur, et al. Selectivity and Mechanism of Fengycin, an Antimicrobial Lipopeptide, from Molecular Dynamics. J Phys Chem B. 2018 Mar 1;122(8):2219-2226.
TN3623	Cepharadione A	Others	Others
	Cepharadione A is a naturally occurring DNA damaging agent.
TN3920	Effusanin A	Raf; Antifection	MAPK; Microbiology/Virology
	Effusanin A 是一种存在于Isodon rugosus 之中的天然产物。它具有 DNA 损伤和抗菌作用。
TN5072	Strictosidine	Others	Others
	Strictosidine has DNA damaging activity in yeast RS 188N mutant, assessed as drug level required to produce 12 mm zone of inhibition.
TN3921	Effusanin B	Antifection	Microbiology/Virology
	Effusanin B shows antibacterial activity. It exhibits DNA-damaging activity in assay which employes DNA-repair deficient (RAD 52Y) and repair proficient (RAD +) yeast strains.

天然产物

Cat.No: T5780

Target: Apoptosis, Parasite, Antifungal

Cat.No: TMS2180

Synonym: Anchovyxanthin,All-Trans-Zeaxanthin,玉米

Target: Antioxidant, Endogenous Metabolite

Cat.No: T0146

Synonym: UK-20349,Vagistat,噻康唑

Target: Antibiotic, Antifection, Antifungal

Trimethylamine N-oxide

Cat.No: T41245

Target: Reactive Oxygen Species, NOD-like Receptor (NLR), TGF-beta/Smad

Cat.No: T37876

Cat.No: TN3623

Target: Others

Cat.No: TN3920

Target: Raf, Antifection

Cat.No: TN5072

Target: Others

Cat.No: TN3921

Target: Antifection

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