K-Ras(G12C) inhibitor 6

mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail

Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.

Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody

Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay

SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.

Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
K-Ras (G12C) inhibitor 6 is an allosterical inhibitor of oncogenic mutation K-Ras G12C [1].
K-Ras (G12C) inhibitor 6 is a cysteine-reactive small molecule. It irreversibly binds to the G12C mutantion of GTPase K-Ras but not the wild-type K-Ras with the relative potency value of 4.2. The binding pocket of K-Ras for K-Ras (G12C) inhibitor 6 is a new allosteric pocket, S-IIP. Binding of this pocket results in a change of the relative nucleotide affinity of Ras to favour GDP over GTP, leading to an accumulation of inactive Ras. Since the mutation of K-Ras is quite common in human cancers, the inhibitor of K-Ras G12C should exert suppression activities in tumor cells. It has been reported that, some of the K-Ras G12C inhibitors are indeed effective to decrease cell viability and increase apoptosis in lung cancer cell lines [1].
References:
[1] Ostrem J M, Peters U, Sos M L, et al. K-Ras (G12C) inhibitors allosterically control GTP affinity and effector interactions. Nature, 2013, 503(7477): 548-551.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 405.34 |
Cas No. | 2060530-16-5 |
Formula | C17H22Cl2N2O3S |
Solubility | ≥20.25mg/mL in DMSO |
SDF | Download SDF |
Canonical SMILES | C1CN(CCC1NC(=O)CCCS)C(=O)COC2=C(C=C(C=C2)Cl)Cl |
Shipping Condition | Evaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request. |
General tips | For obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months. |
Description | K-Ras(G12C) inhibitor 6 is an allosteric, and selective inhibitor of oncogenic K-Ras(G12C). | |||||
Targets | K-Ras(G12C) | |||||
IC50 |
Quality Control & MSDS
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Chemical structure
