2. GPCR/G Protein MAPK/ERK Pathway PI3K/Akt/mTOR
  3. Ras PI3K Akt
  4. VVD-849

VVD-849 is a RAS ligand. VVD-849 covalently binds to Cys242 in the RAS-binding domain of PI3K p110α and promotes RAS/PI3K interaction. VVD-849 partially inhibits pAKT (S473) in HER2-overexpressing tumors. VVD-849 can be used for the research of cancers such as breast cancer.

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

VVD-849

VVD-849 Chemical Structure

CAS No. : 3055321-14-4

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Based on 1 publication(s) in Google Scholar

VVD-849 Related Antibodies

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Akt Akt1 Akt2 Akt3

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

VVD-849 is a RAS ligand. VVD-849 covalently binds to Cys242 in the RAS-binding domain of PI3K p110α and promotes RAS/PI3K interaction. VVD-849 partially inhibits pAKT (S473) in HER2-overexpressing tumors. VVD-849 can be used for the research of cancers such as breast cancer[1][2].

In Vitro

VVD-849 (2 µM; 2 h) exhibits excellent selectivity for cysteine residues in live Jurkat cells[1].
VVD-849 (4 h) enhances the interaction between KRASG12C and p110α in HEK293T cell lysates (cotransfected with p85α), with an IC50 of 0.02 µM[1].
VVD-849 (30 min) increases the level of pAKTS473 in H358 cells, with an IC50 of 0.04 µM[1].
VVD-849 (2 h) partially inhibits the level of pAKT (S473) in N87 (HER2-overexpressing) cells[1].
VVD-849 (1 h) binds to p110α C242 in Jurkat cell lysates, with a TE50 of 0.063 µM[1].
VVD-849 (1 h) shows binding to p110α C242 in Jurkat cell lysates as detected by pocket probe assay, with a TE50 of 0.1 µM[1].
VVD-849 partially inhibits AKT phosphorylation in HER2-overexpressing human gastric cancer N87 cells, which may result from its combined stimulatory effect on the RAS-p110α interaction and inhibitory effect on the HER2-mediated PI3Kα signaling pathway[2].

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

VVD-849 Related Antibodies
Molecular Weight

636.15

Formula

C29H31ClFN3O6S2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

ClC1=CC(C2=CC(OCC3=NC=CC=C3)=CC=C2)=C(S(N4CCC(C(N[C@@H](C)/C=C\S(C)(=O)=O)=O)(F)CC4)(=O)=O)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent & Solubility
In Vitro: 

DMSO : 500 mg/mL (785.98 mM; Need ultrasonic and warming; 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 1.5720 mL 7.8598 mL 15.7196 mL
5 mM 0.3144 mL 1.5720 mL 3.1439 mL
View the Complete Stock Solution Preparation Table

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Purity & Documentation
References

Complete Stock Solution Preparation Table

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.5720 mL 7.8598 mL 15.7196 mL 39.2989 mL
5 mM 0.3144 mL 1.5720 mL 3.1439 mL 7.8598 mL
10 mM 0.1572 mL 0.7860 mL 1.5720 mL 3.9299 mL
15 mM 0.1048 mL 0.5240 mL 1.0480 mL 2.6199 mL
20 mM 0.0786 mL 0.3930 mL 0.7860 mL 1.9649 mL
25 mM 0.0629 mL 0.3144 mL 0.6288 mL 1.5720 mL
30 mM 0.0524 mL 0.2620 mL 0.5240 mL 1.3100 mL
40 mM 0.0393 mL 0.1965 mL 0.3930 mL 0.9825 mL
50 mM 0.0314 mL 0.1572 mL 0.3144 mL 0.7860 mL
60 mM 0.0262 mL 0.1310 mL 0.2620 mL 0.6550 mL
80 mM 0.0196 mL 0.0982 mL 0.1965 mL 0.4912 mL
100 mM 0.0157 mL 0.0786 mL 0.1572 mL 0.3930 mL
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VVD-849 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:

VVD-8493055321-14-4VVD849VVD 849RasPI3KAktPhosphoinositide 3-kinasePKBProtein kinase BRASHEK293T cell lysatesRAS binding domainN87 human gastric cancer cellsAKT phosphorylationH358 cellsHER2cysteine 242PI3K p110αJurkat cellsInhibitorinhibitorinhibit

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