生物活性分子抑制剂RITA(Synonyms: NSC 652287)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。
RITA (Synonyms: NSC 652287) 纯度: 99.45%

RITA 是一种有效的 p53-HDM-2 相互作用抑制剂,可与 p53dN 结合,Kd 值为 1.5 nM,同时能够诱导 DNA-DNA 交联。

RITA(Synonyms: NSC 652287)

RITA Chemical Structure

CAS No. : 213261-59-7

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥770 In-stock
5 mg ¥700 In-stock
10 mg ¥1200 In-stock
50 mg ¥4000 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

RITA 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Cell Cycle/DNA Damage Compound Library
  • Anti-Cancer Compound Library
  • Autophagy Compound Library
  • Anti-Aging Compound Library
  • Ferroptosis Compound Library
  • Pyroptosis Compound Library
  • Glutamine Metabolism Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Transcription Factor Targeted Library
  • Anti-Colorectal Cancer Compound Library

生物活性

RITA is an inhibitor of p53-HDM-2 interaction, binds to p53dN, with a Kd of 1.5 nM, and also induces DNA-DNA cross-links.

IC50 & Target

Kd: 1.5 nM (p53dN)[1]
DNA Crosslinker[2]

体外研究
(In Vitro)

RITA inhibits p53-HDM-2 interaction, binding to p53dN, with a Kd of 1.5 nM. RITA (10 μM) blocks complex formation between p53 and HDM-2 in HCT116 cells and HDFs and in NHF-ERMyc cells irrespective of c-Myc expression. RITA (0.5 μM) reduces the viability of tumor cells in a wild-type p53-dependent manner. Moreover, RITA (0.1 μM) induces p53-dependent apoptosis. RITA induces p53 but does not via DNA damage-signaling pathway[1]. RITA (NSC 652287) induces DNA-DNA cross-links. RITA induces G2-M cell cycle arrest at 10 nM and causes apoptosis at 100 nM. RITA (100 nM) also elevates p53 and causes dose-dependent effects on p21WAF1 protein levels[2]. RITA inhibits the growth of HeLa and CaSki cells, with IC50s of 1 and 10 μM. In addition, RITA (1 μM) stabilizes p53 by inhibiting p53/E6AP interaction[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

RITA (0.1, 1 or 10 mg/kg, i.p.) shows potent antitumor activity in SCID mice bearing HCT116 and HCT116 TP53−/− xenografts[1]. RITA (10 mg/kg, i.p.) also suppresses the growth of HeLa cells in SCID mice[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

292.37

Formula

C14H12O3S2

CAS 号

213261-59-7

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 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 100 mg/mL (342.03 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.4203 mL 17.1016 mL 34.2032 mL
5 mM 0.6841 mL 3.4203 mL 6.8406 mL
10 mM 0.3420 mL 1.7102 mL 3.4203 mL

*

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, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (8.55 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.55 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (8.55 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.55 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (8.55 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.55 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Issaeva N, et al. Small molecule RITA binds to p53, blocks p53-HDM-2 interaction and activates p53 function in tumors. Nat Med. 2004 Dec;10(12):1321-8. Epub 2004 Nov 21.

    [2]. Nieves-Neira W, et al. DNA protein cross-links produced by NSC 652287, a novel thiophene derivative active against human renal cancer cells. Mol Pharmacol. 1999 Sep;56(3):478-84.

    [3]. Zhao CY, et al. Rescue of p53 function by small-molecule RITA in cervical carcinoma by blocking E6-mediated degradation. Cancer Res. 2010 Apr 15;70(8):3372-81.

Cell Assay
[3]

For the cell viability assay, 3,000 cells per well are plated in a 96-well plate and treated with RITA for 48 h, after which cell viability is assessed with the proliferation reagent WST-1. For colony formation assay, cells are seeded in 12-well plates and treated with RITA for 24 h, after which the medium is replaced and the cells are allowed to grow for 10-14 d. The colonies are stained with crystal violet. For growth curves, 3000 cells/mL are plated in 12-well plates, treated with RITA, and counted over 5 d[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice[1]
Female SCID mice, 4-6 weeks old, are implanted with subcutaneous xenografts using 1 × 106 cells in 90% Matrigel. Palpable tumors are established 3-6 d after the cells are injected, at which point RITA treatment is initiated. RITA is administered either 0.1, 1 or 10 mg/kg every day by intravenous or intraperitoneal injection in a total volume of 100 μL phosphate buffered saline. Xenografts are measured every 2 d. Tumor volumes are plotted for control and treated groups by dividing the average tumor volume for each data point by average starting tumor volume[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Issaeva N, et al. Small molecule RITA binds to p53, blocks p53-HDM-2 interaction and activates p53 function in tumors. Nat Med. 2004 Dec;10(12):1321-8. Epub 2004 Nov 21.

    [2]. Nieves-Neira W, et al. DNA protein cross-links produced by NSC 652287, a novel thiophene derivative active against human renal cancer cells. Mol Pharmacol. 1999 Sep;56(3):478-84.

    [3]. Zhao CY, et al. Rescue of p53 function by small-molecule RITA in cervical carcinoma by blocking E6-mediated degradation. Cancer Res. 2010 Apr 15;70(8):3372-81.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

生物活性分子抑制剂RITA(Synonyms: NSC 652287)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

RITA (Synonyms: NSC 652287) 纯度: 99.45%

RITA 是一种有效的 p53-HDM-2 相互作用抑制剂,可与 p53dN 结合,Kd 值为 1.5 nM,同时能够诱导 DNA-DNA 交联。

RITA(Synonyms: NSC 652287)

RITA Chemical Structure

CAS No. : 213261-59-7

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥770 In-stock
5 mg ¥700 In-stock
10 mg ¥1200 In-stock
50 mg ¥4000 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

RITA 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Cell Cycle/DNA Damage Compound Library
  • Anti-Cancer Compound Library
  • Autophagy Compound Library
  • Anti-Aging Compound Library
  • Ferroptosis Compound Library
  • Pyroptosis Compound Library
  • Glutamine Metabolism Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Transcription Factor Targeted Library
  • Anti-Colorectal Cancer Compound Library

生物活性

RITA is an inhibitor of p53-HDM-2 interaction, binds to p53dN, with a Kd of 1.5 nM, and also induces DNA-DNA cross-links.

IC50 & Target

Kd: 1.5 nM (p53dN)[1]
DNA Crosslinker[2]

体外研究
(In Vitro)

RITA inhibits p53-HDM-2 interaction, binding to p53dN, with a Kd of 1.5 nM. RITA (10 μM) blocks complex formation between p53 and HDM-2 in HCT116 cells and HDFs and in NHF-ERMyc cells irrespective of c-Myc expression. RITA (0.5 μM) reduces the viability of tumor cells in a wild-type p53-dependent manner. Moreover, RITA (0.1 μM) induces p53-dependent apoptosis. RITA induces p53 but does not via DNA damage-signaling pathway[1]. RITA (NSC 652287) induces DNA-DNA cross-links. RITA induces G2-M cell cycle arrest at 10 nM and causes apoptosis at 100 nM. RITA (100 nM) also elevates p53 and causes dose-dependent effects on p21WAF1 protein levels[2]. RITA inhibits the growth of HeLa and CaSki cells, with IC50s of 1 and 10 μM. In addition, RITA (1 μM) stabilizes p53 by inhibiting p53/E6AP interaction[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

RITA (0.1, 1 or 10 mg/kg, i.p.) shows potent antitumor activity in SCID mice bearing HCT116 and HCT116 TP53−/− xenografts[1]. RITA (10 mg/kg, i.p.) also suppresses the growth of HeLa cells in SCID mice[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

292.37

Formula

C14H12O3S2

CAS 号

213261-59-7

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 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 100 mg/mL (342.03 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.4203 mL 17.1016 mL 34.2032 mL
5 mM 0.6841 mL 3.4203 mL 6.8406 mL
10 mM 0.3420 mL 1.7102 mL 3.4203 mL

*

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, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (8.55 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.55 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (8.55 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.55 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (8.55 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.55 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Issaeva N, et al. Small molecule RITA binds to p53, blocks p53-HDM-2 interaction and activates p53 function in tumors. Nat Med. 2004 Dec;10(12):1321-8. Epub 2004 Nov 21.

    [2]. Nieves-Neira W, et al. DNA protein cross-links produced by NSC 652287, a novel thiophene derivative active against human renal cancer cells. Mol Pharmacol. 1999 Sep;56(3):478-84.

    [3]. Zhao CY, et al. Rescue of p53 function by small-molecule RITA in cervical carcinoma by blocking E6-mediated degradation. Cancer Res. 2010 Apr 15;70(8):3372-81.

Cell Assay
[3]

For the cell viability assay, 3,000 cells per well are plated in a 96-well plate and treated with RITA for 48 h, after which cell viability is assessed with the proliferation reagent WST-1. For colony formation assay, cells are seeded in 12-well plates and treated with RITA for 24 h, after which the medium is replaced and the cells are allowed to grow for 10-14 d. The colonies are stained with crystal violet. For growth curves, 3000 cells/mL are plated in 12-well plates, treated with RITA, and counted over 5 d[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice[1]
Female SCID mice, 4-6 weeks old, are implanted with subcutaneous xenografts using 1 × 106 cells in 90% Matrigel. Palpable tumors are established 3-6 d after the cells are injected, at which point RITA treatment is initiated. RITA is administered either 0.1, 1 or 10 mg/kg every day by intravenous or intraperitoneal injection in a total volume of 100 μL phosphate buffered saline. Xenografts are measured every 2 d. Tumor volumes are plotted for control and treated groups by dividing the average tumor volume for each data point by average starting tumor volume[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Issaeva N, et al. Small molecule RITA binds to p53, blocks p53-HDM-2 interaction and activates p53 function in tumors. Nat Med. 2004 Dec;10(12):1321-8. Epub 2004 Nov 21.

    [2]. Nieves-Neira W, et al. DNA protein cross-links produced by NSC 652287, a novel thiophene derivative active against human renal cancer cells. Mol Pharmacol. 1999 Sep;56(3):478-84.

    [3]. Zhao CY, et al. Rescue of p53 function by small-molecule RITA in cervical carcinoma by blocking E6-mediated degradation. Cancer Res. 2010 Apr 15;70(8):3372-81.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务