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

RA-9 是一种高效选择性蛋白酶体相关 DUBs 抑制剂，具有良好的毒性和抗癌活性。RA-9 阻断泛素依赖性蛋白降解而不影响 20S 蛋白酶体蛋白水解活性。RA-9 选择性诱导卵巢癌细胞株和供体原代培养细胞凋亡。RA-9 诱导卵巢癌细胞内质网应激反应。

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RA-9

RA-9 Chemical Structure

CAS No. : 919091-63-7

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规格 价格 是否有货 数量
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   询价  
500 mg   询价  

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Customer Review

RA-9 相关抗体

Top Publications Citing Use of Products

查看 Deubiquitinase 亚型特异性产品:

查看所有亚型
USP1 USP2 USP7 USP8 USP10 USP30 UCHL1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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].

细胞效力
(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]
体外研究
(In Vitro)

RA-9 (10-30 μM；48 小时) 抑制卵巢癌细胞系和原代培养物的生长[1]。
RA-9 (1.25-5 μM；18 小时) 导致卵巢癌细胞中的细胞周期停滞和半胱天冬酶介导的细胞凋亡[1]。
RA-9 (5 μM；0-24 小时) 诱导卵巢癌细胞中的内质网应激反应[1]。
RA-9 (5 μM；超过 24 小时) 处理结果与时间依赖性的 PARP 切割形成的积累早在 8 小时就很明显[1]。

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

RA-9 相关抗体:

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.
体内研究
(In Vivo)

RA-9 (5 mg/kg；腹腔注射；服用一天，停药两天) 在卵巢癌小鼠模型中抑制体内人卵巢癌细胞生长并延长存活期[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 号
性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 4.17 mg/mL (11.41 mM; 超声助溶 (<80°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 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
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

RA-9 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 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.

Keywords:

RA-9919091-63-7RA9RA 9DeubiquitinaseApoptosisDUBsovariancancercellsUnfoldedProteinResponsesurvivalERInhibitorinhibitorinhibit

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