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  2. Cell Cycle/DNA Damage Apoptosis
  3. Deubiquitinase Apoptosis
  4. RA-9

RA-9 是一種高效選擇性蛋白酶體相關(guān) DUBs 抑制劑，具有良好的毒性和抗癌活性。RA-9 阻斷泛素依賴性蛋白降解而不影響 20S 蛋白酶體蛋白水解活性。RA-9 選擇性誘導(dǎo)卵巢癌細(xì)胞株和供體原代培養(yǎng)細(xì)胞凋亡。RA-9 誘導(dǎo)卵巢癌細(xì)胞內(nèi)質(zhì)網(wǎng)應(yīng)激反應(yīng)。

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RA-9 Chemical Structure

RA-9 Chemical Structure

CAS No. : 919091-63-7

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規(guī)格 價格 是否有貨 數(shù)量
1 mg ￥160
In-stock
5 mg ￥260
In-stock
10 mg ￥415
In-stock
25 mg ￥738
In-stock
50 mg ￥1148
In-stock
100 mg ￥1813
In-stock
200 mg   詢價  
500 mg   詢價  

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Customer Review

查看 Deubiquitinase 亞型特異性產(chǎn)品:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

RA-9 is a potent and selective proteasome-associated deubiquitinating enzymes (DUBs) inhibitor with favorable toxicity profile and anticancer activity. RA-9 blocks ubiquitin-dependent protein degradation without impacting 20S proteasome proteolytic activity. RA-9 selectively induces onset of apoptosis in ovarian cancer cell lines and primary cultures derived from donors. RA-9 induces endoplasmic reticulum (ER)-stress responses in ovarian cancer cells[1].

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
0.4 μM
Compound: 4c
Cytotoxicity against human A549 cells after 72 hrs by MTT assay
Cytotoxicity against human A549 cells after 72 hrs by MTT assay
[PMID: 19046794]
Caov-3 cell line IC50
1.03 μM
Compound: 4c
Cytotoxicity against human Caov3 cells after 72 hrs by MTT assay
Cytotoxicity against human Caov3 cells after 72 hrs by MTT assay
[PMID: 19046794]
HepG2 IC50
> 2000 ng/mL
Compound: 5b
Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay
Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay
[PMID: 24139941]
HepG2 IC50
356 ng/mL
Compound: 5b
Antimalarial activity against liver stage Plasmodium berghei ANKA sporozoites infected in human HepG2 cells after 48 hrs by luciferase reporter gene assay
Antimalarial activity against liver stage Plasmodium berghei ANKA sporozoites infected in human HepG2 cells after 48 hrs by luciferase reporter gene assay
[PMID: 24139941]
HL-60 CC50
3.6 μM
Compound: 1c
Cytotoxicity against human HL60 cells in presence of RPMI1640 containing 10% fetal bovine serum by trypan blue exclusion test
Cytotoxicity against human HL60 cells in presence of RPMI1640 containing 10% fetal bovine serum by trypan blue exclusion test
[PMID: 17499885]
HSC-2 CC50
0.9 μM
Compound: 1c
Cytotoxicity against human HSC2 by MTT method
Cytotoxicity against human HSC2 by MTT method
[PMID: 17499885]
HSC-4 CC50
6.1 μM
Compound: 1c
Cytotoxicity against human HSC4 cells by MTT method
Cytotoxicity against human HSC4 cells by MTT method
[PMID: 17499885]
PC-3 IC50
1.54 μM
Compound: 4c
Cytotoxicity against human PC3 cells after 72 hrs by MTT assay
Cytotoxicity against human PC3 cells after 72 hrs by MTT assay
[PMID: 19046794]
SK-OV-3 IC50
2.5 μM
Compound: 4c
Cytotoxicity against human Scov3 cells after 72 hrs by MTT assay
Cytotoxicity against human Scov3 cells after 72 hrs by MTT assay
[PMID: 19046794]
U-87MG ATCC IC50
7.15 μM
Compound: 2e
Cytotoxicity against human U87MG cells after 48 hrs by resazurin assay
Cytotoxicity against human U87MG cells after 48 hrs by resazurin assay
[PMID: 25639862]
體外研究
(In Vitro)

RA-9 (10-30 μM；48 小時) 抑制卵巢癌細(xì)胞系和原代培養(yǎng)物的生長[1]。
RA-9 (1.25-5 μM；18 小時) 導(dǎo)致卵巢癌細(xì)胞中的細(xì)胞周期停滯和半胱天冬酶介導(dǎo)的細(xì)胞凋亡[1]。
RA-9 (5 μM；0-24 小時) 誘導(dǎo)卵巢癌細(xì)胞中的內(nèi)質(zhì)網(wǎng)應(yīng)激反應(yīng)[1]。
RA-9 (5 μM；超過 24 小時) 處理結(jié)果與時間依賴性的 PARP 切割形成的積累早在 8 小時就很明顯[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: Cisplatin-sensitive ovarian cancer cell lines TOV-21G and ES-2, Cisplatin-resistant ovarian cancer cell lines HEY and OVCAR-3, primary ovarian cancer cells
Concentration: 10, 20, 30 μM
Incubation Time: 48 hours
Result: Compromised the viability of ovarian cancer cells in a dose-dependent fashion.

Cell Cycle Analysis[1]

Cell Line: ES-2 cells
Concentration: 1.25, 5 μM
Incubation Time: 18 hours
Result: Resulted in a dose-dependent increase in the fraction of ES-2 cells in the G2-M cell cycle phase.

Western Blot Analysis[1]

Cell Line: ES-2, SKOV-3 and TOV-21G ovarian cancer cells
Concentration: 5 μM
Incubation Time: 0-24 h
Result: Caused a time-dependent increase in the steady levels of the early ER-stress marker GRP-78, as well as the late ER-stress markers IRE1-α and Ero1L-α.
體內(nèi)研究
(In Vivo)

RA-9 (5 mg/kg；腹腔注射；服用一天，停藥兩天) 在卵巢癌小鼠模型中抑制體內(nèi)人卵巢癌細(xì)胞生長并延長存活期[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Six-week-old female immunodeficient (NCr nu/nu) mice[1]
Dosage: 5 mg/kg
Administration: I.p; one-day on, two-days off
Result: Significant reduction in tumor burden at day 12.
分子量

365.34

Formula

C19H15N3O5
CAS 號
性狀

固體

顏色

Light yellow to yellow

運輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細(xì)胞實驗： 

DMSO 中的溶解度 : 4.17 mg/mL (11.41 mM; 超聲助溶 (<80°C); 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.7372 mL 13.6859 mL 27.3718 mL
5 mM 0.5474 mL 2.7372 mL 5.4744 mL
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(nèi)使用。

  • 摩爾計算器

  • 稀釋計算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質(zhì)量
=
濃度
×
體積
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物溶解方案計算器
請輸入動物實驗的基本信息：

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

只
由于實驗過程有損耗，建議您多配一只動物的量
計算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料
參考文獻(xiàn)

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7372 mL 13.6859 mL 27.3718 mL 68.4294 mL
5 mM 0.5474 mL 2.7372 mL 5.4744 mL 13.6859 mL
10 mM 0.2737 mL 1.3686 mL 2.7372 mL 6.8429 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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產(chǎn)品名稱：
RA-9
目錄號：
HY-136528
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