2. Membrane Transporter/Ion Channel MAPK/ERK Pathway GPCR/G Protein Autophagy Apoptosis
  3. Proton Pump Ras Autophagy Apoptosis
  4. RSC-1255

RSC-1255 是一种高效且选择性的 V-ATPase 抑制剂，可直接结合哺乳动物 V-ATPase 复合物，结合常数 Kd 为 23 nM。RSC-1255 对 KRAS 突变型癌细胞具有更高的选择性细胞毒性，尤其对 KRASG13D 和 KRASG12V细胞表现最为敏感。RSC-1255 能阻断溶酶体酸化 (lysosomal acidification)、自噬 (autophagy) 以及巨胞饮 (macropinocytosis) 过程。RSC-1255 可用于 KRAS 驱动的肺癌和结直肠癌研究。

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RSC-1255

RSC-1255 Chemical Structure

CAS No. : 2171015-78-2

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RSC-1255 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

RSC-1255 is a potent and selective Vacuolar H⁺-ATPase (V-ATPase) inhibitor that directly binds the mammalian V-ATPase complex with a Kd = 23 nM. RSC-1255 exhibits preferential cytotoxicity toward KRAS-mutant cancer cells, especially KRASG13D and KRASG12V cells. RSC-1255 blocks lysosomal acidification, autophagy, and macropinocytosis in cancer cells. RSC-1255 can be used for the study of KRAS-driven lung and colon cancers[1].

IC50 & Target[1]

KRAS G13D

 

KRas G12V

 

体外研究
(In Vitro)

RSC-1255 (249C) (1 μM；1 小时) 在 HEK293T 细胞中抑制 V-ATPase 介导的质子泵功能和溶酶体酸化[1]。
RSC-1255 (1 μM；1 小时) 在 HEK293T 细胞中改变 V-ATPase 组装，增加膜相关 V1 亚基水平[1]。
RSC-1255 在人源癌细胞系中表现出强效的细胞生长抑制活性，其 IC50 值分别为：A549 （KRAS 突变） 0.073 μM、LOX IMVI ( BRAFV600E) 0.06 μM、MelJuso ( HRASG13D/NRASQ61L) 0.022 μM[1]。
RSC-1255 (0-10 μM；72 小时) 在 KRAS 突变型 MEF 中选择性降低细胞活力，其中 KRASG13D 和 KRASG12V 细胞最敏感[1]。
RSC-1255 (1 μM；2 , 4 , 8 , 20 , 24 小时) 在 A549 细胞中阻断自噬通量，并以时间依赖性方式升高 SQSTM1/p62 和 LC3-II 水平[1]。
RSC-1255 (1 μM；1小时) 可升高 KRASG13D MEF 的溶酶体 pH，逆转其高度酸性的基础状态[1]。
RSC-1255 (1 μM；1小时) 在 FITC 负载的溶酶体中抑制 V-ATPase 依赖的质子转运，其中 KRASG13D MEF 的抑制最为显著[1]。
RSC-1255 (1 μM；24小时) 增大自噬囊泡尺寸，并在 KRASG13D、KRASG12V 及 BRAFV600E MEF 中阻断溶酶体–自噬体融合[1]。
RSC-1255 (1 μM；2小时) 显著降低 MEF 中的巨胞饮水平，其中 KRASG13D 细胞的抑制效果最强[1]。
RSC-1255 (1 μM；24 小时) 可诱导 KRAS 突变型 MEF 发生凋亡，其中 KRASG13D、KRASG12V 及 BRAFV600E 细胞的 Annexin V⁺ / PI⁺ 水平最高[1]。

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

RSC-1255 相关抗体:

Western Blot Analysis[1]

Cell Line: HEK293T cells
Concentration: 1 μM
Incubation Time: 1h
Result: Increased membrane-associated V1 subunit B2 was observed, indicating altered V-ATPase assembly after treatment.

Western Blot Analysis[1]

Cell Line: A549 cells
Concentration: 1 μM
Incubation Time: 2 , 4 , 8 , 20 , 24 h
Result: Time-dependent accumulation of SQSTM1/p62 and LC3-II, indicating autophagic flux inhibition.

Cell Viability Assay[1]

Cell Line: MEF KRAS mutants (KRASG13D, KRASG12V, KRASG12D, KRASG12S, KRASG12C, KRASQ61L, KRASQ61R, WT)
Concentration: 0-10 μM
Incubation Time: 72 h
Result: Highest sensitivity in KRASG13D and KRASG12V MEFs with the lowest IC50 values; minimal sensitivity in WT MEFs.

Apoptosis Analysis[1]

Cell Line: MEFs expressing KRASG13D, KRASG12V, BRAFV600E and other KRAS mutants
Concentration: 1 μM
Incubation Time: 24h
Result: Increased of Annexin V+/PI+ apoptotic cells, with KRASG13D,KRASG12V and BRAFV600E MEFs showing the strongest apoptotic responses.
体内研究
(In Vivo)

RSC-1255 (249 C) (10 mg/kg；腹腔注射 (i.p.)；每日一次或两次) 在 KRAS 突变型肺癌和结直肠癌异种移植模型中显著抑制肿瘤生长[1]。

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

Animal Model: A549 (KRASG12S) lung cancer xenografts were established in five-week-old athymic mice.
Dosage: 10 mg/kg
Administration: Intraperitoneal injection (i.p.); twice daily
Result: Significantly reduced tumor volumes in A549 xenograft-bearing mice during the treatment period.
Increased LC3-I/II levels in tumor tissues, indicating autophagy inhibition in vivo.
No significant systemic toxicity, with normal body weight, organ weights and hematological parameters.
Animal Model: SW48 xenograft models bearing parental or KRAS-mutant SW48 cells (KRASG12D/+, KRASG12V/+, KRASG13D/+) were established in five-six-week-old athymic mice].
Dosage: 10 mg/kg
Administration: Intraperitoneal injection (i.p.); 2 weeks.
Result: Significant tumor growth inhibition in KRAS-mutant SW48 xenografts, with the strongest effects in KRASG13D/+ and KRASG12V+ tumors.
Minimal response in parental SW48 tumors, consistent with lower in vitro sensitivity.
No significant changes in body weight or systemic toxicity during treatment.
分子量

564.96

Formula

C27H25ClF4N4O3
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

RSC-1255 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • 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:

RSC-12552171015-78-2RSC1255RSC 1255Proton PumpRasAutophagyApoptosisV-ATPase inhibitorKRAS-mutant cellsautophagy inhibitionapoptosis inductionlung cancercolon cancerInhibitorinhibitorinhibit

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