1. GPCR/G Protein
  2. Ras
  3. KRA-533

KRA-533 

Cat. No.: HY-138188
Handling Instructions

KRA-533 is a potent KRAS agonist. KRA-533 binds to the GTP/GDP binding pocket in the KRAS protein to prevent GTP cleavage, resulting in the accumulation of constitutively active GTP-bound KRAS that triggers both apoptotic and autophagic cell death pathways in cancer cells.

For research use only. We do not sell to patients.

KRA-533 Chemical Structure

KRA-533 Chemical Structure

CAS No. : 10161-87-2

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Description

KRA-533 is a potent KRAS agonist. KRA-533 binds to the GTP/GDP binding pocket in the KRAS protein to prevent GTP cleavage, resulting in the accumulation of constitutively active GTP-bound KRAS that triggers both apoptotic and autophagic cell death pathways in cancer cells.

IC50 & Target

KRAS[1]

In Vitro

KRA-533 (10 μM; 48 hours; HCC827 cells) enhances KRAS activity to a greater extent[1].
KRA-533 (0~15 μM; 48 hours; H157 cells) enhances KRAS activity in a dose-dependent manner, which is associated increased levels of pERK, ratio of active caspase 3/procaspase 3 and PARP cleavage, leading to apoptotic cell death[1].
KRA-533 (10 μM; 10 days; H292 cells) mediates cell growth suppression than those without KRAS mutation. KRA-533 (5~15 μM) can directly bind to WT, G12C, G12D and G13D mutant KRAS proteins. KRA-533 activates WT KRAS to increase its activity in a dose-dependent manner. KRA-533 further enhances the activities of active KRAS mutants[1].

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

Western Blot Analysis[1]

Cell Line: HCC827 cells
Concentration: 10 μM
Incubation Time: 48 hours
Result: Enhanced KRAS activity to a greater extent.

Apoptosis Analysis[1]

Cell Line: H157 cells
Concentration: 0~15 μM
Incubation Time: 48 hours
Result: Enhanced KRAS activity in a dose-dependent manner, which was associated increased levels of pERK, ratio of active caspase 3/procaspase 3 and PARP cleavage, leading to apoptotic cell death.
In Vivo

KRA-533 (0~30 mg/kg; 28 days) suppresses tumor growth in a dose-dependent manner in lung cancer mutant KRAS xenografts and induces apoptosis and autophagy in tumor tissues in a dose-dependent manner[1].
KRA-533 shows optimal therapeutic index between 7.5 mg/kg and 30 mg/kg doses[1].

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

Animal Model: Nu/Nu nude mice[1]
Dosage: 0~30 mg/kg
Administration: I.p.
Result: Suppressed tumor growth in a dose-dependent manner in lung cancer mutant KRAS xenografts and induced apoptosis and autophagy in tumor tissues in a dose-dependent manner.
Molecular Weight

314.18

Formula

C₁₃H₁₆BrNO₃

CAS No.
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KRA-533
Cat. No.:
HY-138188
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