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細胞週期與DNA損傷 Cell cycle and DNA damage 細胞週期與DNA損傷 Cell cycle and DNA damage

細胞週期與DNA損傷 Cell cycle and DNA damage

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細胞週期與DNA損傷 Cell cycle and DNA damage
細胞週期與DNA損傷 Cell cycle and DNA damage



細胞週期 Cell cycle

在細胞週期 (cell cycle) 中是透過週期蛋白依賴性激酶或週期素依賴性激酶(cyclin-dependent
kinases, CDKs) 來調控細胞生長 (cell growth)、DNA 複製 (DNA replication) 與細胞分裂 (cell division) 的所有過程。在整個細胞週期中有幾個檢查站 (checkpoint),為錯誤的訊息或是訊號把關,例如:DNA 損傷、紡錘體 (spindle) 形成不當等,確保細胞週期能夠持續運轉。當細胞週期運轉異常時,可能會造成細胞異常增殖與基因組的不穩定性,最終導致癌症細胞的產生。

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品名分析内容貨號
Cell cycle assay kit· Easy-to-use kit for flow cytometric analysis of cell cycle progression
· Determine the percentage of cells in G0/G1, G2, or S phase
10009349
Senescence-Associated β-Galactosidase Staining Kit· Enables visual detection of senescent cells using a chromogenic substrate602010


週期蛋白依賴性激酶 CDKs

CDKs 激酶與特定的細胞週期蛋白因子共同調控細胞週期中各個階段。當CDKs 激酶功能異常時則會引發癌症細胞的產生。不同的CDKs 激酶與其因子調控的階段如下:
  Cdk4/cyclin D 和Cdk6/cyclin D:G1 phase
  Cdk2/cyclin E:S phase 初期
  Cdk1/cyclin A 和Cdk2/cyclin A:S phase
  Cdk1/cyclin B:有絲分裂 (mitosis)

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貨號 品名 活性
21765 Butyrolactone I An ATP-competitive inhibitor of Cdk1 (IC50 = 20 μg/ml in PC-14 cells); induces dose-dependent G2/M arrest, inhibits DNA synthesis, and decreases Cdk1 protein expression in vitro
18859 Cdk1/2 Inhibitor III A cell-permeable inhibitor of Cdk1/cyclin B and Cdk2/cyclin A (IC50s = 0.6 and 0.5 nM, respectively)
17666 LEE011 Targets Cdk4/cyclin D1 and Cdk6/cyclin D3 at nanomolar concentrations; prevents CDK-mediated G1/S phase transition, arresting the cell cycle in the G1 phase, suppressing DNA synthesis, and inhibiting cancer cell growth
21560 LY2835219 Orally bioavailable dual inhibitor of Cdk4 and Cdk6 (IC50s = 2 and 10 nM, respectively); induces G1 arrest
13317 NU 6102 Inhibits Cdk1 and Cdk2 (IC50s = 9.5 and 5.4 nM, respectively); delays cell entry into mitosis
21474 PHA-848125 An ATP-competitive inhibitor of Cdk2/cyclin A (IC50 = 45 nM); at least 3-fold less potent at Cdk1, -3, -4, -5, and -7
16273 PD 0332991 (hydrochloride) An orally active, selective inhibitor of Cdk4 (IC50 = 11 nM) and Cdk6 (IC50= 16 nM); induces G1 arrest
15149 Ro 3306 A cell-permeable, reversible inhibitor of Cdk1; selective for Cdk1/cyclin B1 (Ki = 35 nM) over Cdk1/cyclin A (Ki = 110 nM); induces reversible cell cycle arrest at the G2/M phase border
10009569 (R)-Roscovitine An inhibitor of Cdk2/cyclin E (IC50 = 0.1 μM); also inhibits Cdk7/cyclin H, Cdk5/p35, and cell division cycle (cdc)/cyclin B (IC50s = 0.49, 0.16, and 0.65 μM, respectively)


DNA 損傷劑 DNA damaging agents

內源性的壓力來源 :活性氧類 (ROS)、拓璞異構酵素抑制劑 (topoisomerase inhibitors)、DNA 烷化劑 (DNA alkylating)或交聯劑 crosslinking agents,以及核苷類似物 (nucleoside analogs)等皆有可能會造成DNA 損傷,進而影響細胞週期。 臨床上使用的化療藥物,是透過S phase 的活化來引發DNA 損傷,進而抑制癌症細胞DNA 的複
製,促進癌症細胞的老化與凋亡,抑制癌症細胞的生長。

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DNA Topoisomerase Inhibitors
DNA 單股或雙股螺旋的裂解可以透過抑制DNA topoisomerase 酵素活性完成
貨號 品名
11694 Camptothecin
15007 Doxorubicin (hydrochloride)
12092 Etoposide
14180 Irinotecan (hydrochloride hydrate)
14129 Topotecan (hydrochloride)
DNA Crosslinking Agents
含鉑 (platinum) 的DNA 交聯劑與DNA 或是DNA 蛋白交聯,干擾DNA 和RNA 的生成
貨號 品名
13112 Carboplatin
13119 Cisplatin
29001 Nedaplatin
13106 Oxaliplatin
DNA Alkylating Agents
烷基與DNA 鹼基對反應,誘導DNA 雙股螺旋鍵接的分裂,抑制細胞分裂,促進細胞死亡
貨號 品名
23693 Bendamustine (hydrochloride)
19527 4-hydroperoxy Cyclophosphamide
16665 Melphalan
11435 Mitomycin C
14163 Temozolomide
Nucleoside Analogs
這些抗癌劑可以在復製過程中結合到 DNA 中,導致複製叉停滯和鏈終止。多種核苷類似物也抑制關鍵的細胞酶
貨號 品名
16069 Cytarabine
14154 Floxuridine
14128 Fludarabine
14416 5-Fluorouracil
11690 Gemcitabine
21366 Trifluorothymidine



DNA 損傷檢查站與修復 DNA Damage Checkpoints & Repair

DNA 損傷的檢測可以激活G1 期、S 期和G2/M 過渡期的細胞週期檢查點,以阻止細胞週期並進行DNA 修復。當DNA 複製壓力增加時,Ataxia-telangiectasia 和Rad3 相關蛋白/ 激酶 (ATR) 會被激活,使單股斷裂;而當Ataxia-telangiectasia mutated kinase (ATM) 活化時,則使雙股螺旋斷裂。ATR 和ATM 也會個別活化Chk1 和Chk2 激酶,進而調控下游的CDK/cyclin complexes 與細胞週期的運轉。透過抑制ATR/ATM-Chk1/Chk2 路徑,Wee1 蛋白或是DNA 修復酵素可以加劇DNA 的損傷,促進細胞減數分裂,最終導致有細胞死亡或衰老。

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ATM inhibitors
貨號 品名
25648 AZD 0156
16336 Ku-55933
17502 Ku-60019
ATR inhibitors
貨號 品名
17589 AZ 20
21035 AZD 6738
17587 VE-821
Wee1 Inhibitors
貨號 品名
21266 MK-1775
35391 Wee1 Inhibitor
DNA Ligase Inhibitors
貨號 品名
18374 L189
22941 L67
18015 SCR7
Chk1 Inhibitors
貨號 品名
34300 GDC-0575
20351 LY2603618
21490 LY2606368
17859 PF-477736
18131 SCH 900776
18130 UCN-01
Chk2 Inhibitors
貨號 品名
19178 CCT241533 (hydrochloride)
21184 Chk2 Inhibitor
19811 NSC 109555
PARP1 Inhibitors
貨號 品名
11505 ABT-888 (hydrochloride)
19782 BMN 673
20842 MK-4827 (tosylate)
10621 Olaparib
33182 Pamiparib
15643 Rucaparib


紡錘體組裝檢查點 Spindle Assembly Checkpoint

當有絲分裂期間存在未連接或不正確連接的著絲點 (kinetochores) 時,紡錘體檢查點 (spindle checkpoint) 被激活,進而抑制促後期複合體 (anaphase-promoting complex/cyclosome, APC/C),且避免細胞週期進展至後期階段。Mad2、BubR1、Bub3 以及 APC/C 共激活因子 - Cdc20 聚集在有絲分裂檢查點複合體 (mitotic checkpoint complex),與激酶: Bub1、Mps1、Aurora B和 Plk1 共同參與 SAC 的調節。

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Mitotic Checkpoint Complex Modulators
貨號 品名
17080 Apcin
22297 M2I-1
17550 N-4-Tosyl-L-arginine methyl ester (hydrochloride)
25835 proTAME
Mps1 Inhibitors
貨號 品名
19991 AZ 3146
21660 BAY 12-17389
19175 Mps1-IN-1
25554 Mps1/TTK Inhibitor
31613 NMS-P715
10004412 Reversine
Plk1 Inhibitors
貨號 品名
17385 BI-2536
18193 BI-6727
18099 GSK461364
15553 ON-01910 (sodium salt)
21669 Ro 3280
Aurora B Inhibitors
貨號 品名
13647 AZD 1152 (hydrochloride)
11602 AZD 1152-HQPA
24199 Hesperadin
13601 ZM 447439


Modulators of Microtubule Dynamics

微管抑製劑(microtubule inhibitors) 結合β- 微管蛋白 (β-tubulin), 影響微管動力學和有絲分裂紡錘體结合, 活化紡錘體組裝檢查點。紫杉醇類 (Taxanes) 穩定微管(preexisting
microtubules), 而長春花生物鹼 (Vinca alkaloids) 則防止微管聚合 (microtubules polymerization)。

Taxanes
貨號 品名
22262 Cabazitaxel
11637 Docetaxel (hydrate)
10461 Paclitaxel
20741 7-epi Paclitaxel
Vinca Alkaloids
貨號 品名
11762 Vinblastine (sulfate)
11764 Vincristine (sulfate)
21262 Vinorelbine (tartrate)


其他相關試劑盒 

貨號 品名
700160 Myeloperoxidase (MPO) Peroxidation Fluorometric Assay Kit
10006438 Myeloperoxidase (MPO) Chlorination Fluorometric Assay Kit
600450 Glycolysis Cell-Based Assay Kit
700470 Pyruvate Assay Kit
700510 L-Lactate Assay Kit
10011725 Glycerol Cell-Based Assay Kit
701350 α-Ketoglutarate Fluorometric Detection Assay Kit
10006908 Adipogenesis Assay Kit
10009381 Adipolysis Assay Kit
701490 Deubiquitinases (DUB) Activity Assay Kit
703202 Glutathione Reductase Assay Kit
703102 Glutathione Peroxidase Assay Kit



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發佈者 發佈時間 Apr 15, 2022 瀏覽次數 526
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