2. GPCR/G Protein MAPK/ERK Pathway Stem Cell/Wnt PI3K/Akt/mTOR
  3. Ras MEK ERK Akt
  4. SHY-855

SHY-855 is a pan RAS inhibitor. SHY-855 effectively prevents the binding of K-Ras proteins and other members of the Ras superfamily of small GTPases with IC50 values of 0.3-5 μM. SHY-855 effectively inhibits the phosphorylation of MEK, ERK1/2, and AKT downstream of K-Ras. SHY-855 inhibits the formation of the Ras-GTP activity complex. SHY-855 can be used to the studies of pancreatic cancer and non-small cell lung cancer.

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SHY-855

SHY-855 Chemical Structure

CAS No. : 2446485-15-8

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SHY-855 Related Antibodies

Top Publications Citing Use of Products

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MEK1 MEK2 MEK5 MEK MAP2K4/MEK4 MAP2K7/MEK7

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ERK ERK1 ERK2 ERK5 ERK8

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Akt Akt1 Akt2 Akt3

  • Biological Activity

  • Purity & Documentation

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  • Customer Review

Description

SHY-855 is a pan RAS inhibitor. SHY-855 effectively prevents the binding of K-Ras proteins and other members of the Ras superfamily of small GTPases with IC50 values of 0.3-5 μM. SHY-855 effectively inhibits the phosphorylation of MEK, ERK1/2, and AKT downstream of K-Ras. SHY-855 inhibits the formation of the Ras-GTP activity complex. SHY-855 can be used to the studies of pancreatic cancer and non-small cell lung cancer[1].

IC50 & Target[1]

K-Ras WT

2.5 μM (IC50)

KRas G12D

2.5 μM (IC50)

KRas G12C

3 μM (IC50)

KRas Q61H

5 μM (IC50)

MEK

 

ERK1

 

ERK2

 

Akt

 

In Vitro

SHY-855 competes with GTP binding to K-Ras WT, the G12D, G12C, and Q61H mutants, as well as Rac-1, Rho-A, Rab5, and Rab35 with IC50s of 2.5, 2.5, 3, 5, 2.5, 2.5, 0.3 and 0.6 μM[1].
SHY-855 (72 h) exhibits potent antiproliferative effects in multiple tumor cell lines, including pancreatic cancer (PANC-1, MIA PaCa-2, BxPC3) and non-small cell lung cancer (NCI-H1975, A549, NCI-H1299), with IC50 values ranging from 0.75-2.9 μM[1].
SHY-855 (0.3-10 μM, 6 h) significantly inhibits the phosphorylation of key signaling molecules induced by EGF in PANC-1, MIA PaCa-2 and NCI-H1975 cells[1].
SHY-855 (1.25-10 μM, 6 h) inhibits Ras-GTP complex formation with an IC50 of 1-3 μM in PANC-1, MIA PaCa-2 and NCI-H1975 cells[1].

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

SHY-855 Related Antibodies

Western Blot Analysis[1]

Cell Line: PANC-1, MIA PaCa-2 and NCI-H1975 cells
Concentration: 0.3, 0.6, 1.25, 2.5, 5 and 10 μM
Incubation Time: 6 h
Result: Inhibited phosphorylation and activation of MEK, Erk1/2, and Akt in PANC-1, MIA PaCa-2, and NCIH1975 cell lines in a dose-dependent manner with similar IC50 values (about 1-3 μM).
Prevented Ras-GTP complex formation with IC50 values in the range of 1 to 3 μM.
Molecular Weight

506.02

Formula

C26H24ClN5O2S
CAS No.
Appearance

Solid

Color

Light yellow to light brown

SMILES

COCCNC1=NC(C2=NC=CN2C)=NC3=C1C(C4=CC=CC=C4)=C(S3)C5=C(C(OC)=CC=C5)Cl
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
Solvent & Solubility
In Vitro: 

DMSO : 33.33 mg/mL (65.87 mM; ultrasonic and warming and heat to 60°C; 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 1.9762 mL 9.8810 mL 19.7621 mL
5 mM 0.3952 mL 1.9762 mL 3.9524 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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C2

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V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 3.33 mg/mL (6.58 mM); Clear solution

    This protocol yields a clear solution of ≥ 3.33 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (33.3 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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 1.9762 mL 9.8810 mL 19.7621 mL 49.4052 mL
5 mM 0.3952 mL 1.9762 mL 3.9524 mL 9.8810 mL
10 mM 0.1976 mL 0.9881 mL 1.9762 mL 4.9405 mL
15 mM 0.1317 mL 0.6587 mL 1.3175 mL 3.2937 mL
20 mM 0.0988 mL 0.4941 mL 0.9881 mL 2.4703 mL
25 mM 0.0790 mL 0.3952 mL 0.7905 mL 1.9762 mL
30 mM 0.0659 mL 0.3294 mL 0.6587 mL 1.6468 mL
40 mM 0.0494 mL 0.2470 mL 0.4941 mL 1.2351 mL
50 mM 0.0395 mL 0.1976 mL 0.3952 mL 0.9881 mL
60 mM 0.0329 mL 0.1647 mL 0.3294 mL 0.8234 mL
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SHY-855 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:

SHY-8552446485-15-8SHY855SHY 855RasMEKERKAktMitogen-activated protein kinase kinaseMAPKKMAP2KExtracellular signal regulated kinasesPKBProtein kinase BPANC-1MIA PaCa-2NCI-H1975 K-Ras WT and mutantsRas-GTP complexInhibitorinhibitorinhibit

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