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

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 induces apoptosis and blocks lysosomal acidification, autophagy, and macropinocytosis in cancer cells. RSC-1255 can be used for the study of KRAS-driven lung and colon cancers.

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RSC-1255

RSC-1255 Chemical Structure

CAS No. : 2171015-78-2

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Based on 1 publication(s) in Google Scholar

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Description

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 induces apoptosis and 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

 

In Vitro

RSC-1255 (249C) (1 μM; 1 h) inhibits V-ATPase–mediated proton pumping and lysosomal acidification in HEK293T cells[1].
RSC-1255 (1 μM; 1 h) disrupts V-ATPase assembly by increasing membrane-associated V1 subunits in HEK293T cells[1].
RSC-1255 exhibits potent growth-inhibitory activity in human cancer cell lines, with IC50 values of 0.073 μM in A549 (KRAS-mutant), 0.06 μM in LOX IMVI (BRAFV600E), and 0.022μM in MelJuso (HRASG13D/NRASQ61L) cells[1].
RSC-1255 (0-10 μM; 72 h) selectively reduces cell viability in KRAS-mutant mouse embryonic fibroblasts (MEFs) with the highest sensitivity in KRASG13D and KRASG12V cells[1].
RSC-1255 (1 μM; 2-24 h) blocks autophagic flux, increasing SQSTM1/p62 and LC3-II accumulation in A549 cells[1].
RSC-1255 (1 μM; 1 h) increases lysosomal pH in KRASG13D MEFs, reversing their highly acidic basal lysosomal state[1].
RSC-1255 (1 μM; 1 h) inhibits V-ATPase–dependent proton transport in FITC-loaded lysosomes, showing the strongest inhibition in KRASG13D MEFs[1].
RSC-1255 (1 μM; 24 h) enlarges autophagic vesicles and blocks lysosome-autophagosome fusion in KRASG13D, KRASG12V and BRAFV600E MEFs[1].
RSC-1255 (1 μM; 2 h) markedly reduces macropinocytosis levels in MEFs, with KRASG13D cells showing the strongest suppression[1].
RSC-1255 ((1 μM; 24 h) induces apoptosis in KRAS-mutant MEFs, with KRASG13D, KRASG12V and BRAFV600E cells showing the highest Annexin V⁺/PI⁺levels[1].

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

RSC-1255 Related Antibodies

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.
In Vivo

RSC-1255 (249C) (10 mg/kg; intraperitoneal (i.p.) injection; once or twice daily) significantly inhibits tumor growth in KRAS-mutant lung cancer and KRAS-mutant colorectal cancer xenograft models in mice[1].

MedChemExpress (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.
Clinical Trial
Molecular Weight

564.96

Formula

C27H25ClF4N4O3
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(C1(C)N(C2=CC=C(C=C2F)F)N=C(C1C3=CC=C(Cl)O3)C4=C(F)C=C(F)C=C4)NCC5OCCN(C5)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation
References
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    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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