2. GPCR/G Protein MAPK/ERK Pathway
  3. Ras
  4. KRA-533

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.

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KRA-533 Chemical Structure

KRA-533 Chemical Structure

CAS No. : 10161-87-2

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Based on 1 publication(s) in Google Scholar

KRA-533 Related Antibodies

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K-Ras H-Ras N-Ras Ras

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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].

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

KRA-533 Related Antibodies

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; i.p.; 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].

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

Animal Model: Nu/Nu nude mice (mutant KRAS xenografts)[1]
Dosage: 0~30 mg/kg
Administration: i.p.; 28 days
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.
Appearance

Solid

Color

White to off-white

SMILES

O=C(O)C1=CC=C(CCCCNC(CBr)=O)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (795.72 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1829 mL 15.9144 mL 31.8289 mL
5 mM 0.6366 mL 3.1829 mL 6.3658 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Working solution concentration: mg/mL
Purity & Documentation

Purity: 98.94%

SDS (251 KB)

COA (242 KB) HNMR (268 KB) LCMS (271 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.1829 mL 15.9144 mL 31.8289 mL 79.5722 mL
5 mM 0.6366 mL 3.1829 mL 6.3658 mL 15.9144 mL
10 mM 0.3183 mL 1.5914 mL 3.1829 mL 7.9572 mL
15 mM 0.2122 mL 1.0610 mL 2.1219 mL 5.3048 mL
20 mM 0.1591 mL 0.7957 mL 1.5914 mL 3.9786 mL
25 mM 0.1273 mL 0.6366 mL 1.2732 mL 3.1829 mL
30 mM 0.1061 mL 0.5305 mL 1.0610 mL 2.6524 mL
40 mM 0.0796 mL 0.3979 mL 0.7957 mL 1.9893 mL
50 mM 0.0637 mL 0.3183 mL 0.6366 mL 1.5914 mL
60 mM 0.0530 mL 0.2652 mL 0.5305 mL 1.3262 mL
80 mM 0.0398 mL 0.1989 mL 0.3979 mL 0.9947 mL
100 mM 0.0318 mL 0.1591 mL 0.3183 mL 0.7957 mL
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KRA-533 Related Classifications

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:

KRA-53310161-87-2KRA533KRA 533RaspotentGTP/GDPcleavageGTP-boundapoptoticautophagiccancerInhibitorinhibitorinhibit

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