PPI-GIT1/β-Pix interaction-IN-1

Name: PPI-GIT1/β-Pix interaction-IN-1
Brand: MedChemExpress
SKU: HY-152095
Rating: 4.5 (1 reviews)

Cat. No.: HY-152095 Purity: 98.63%: FAQs
Data Sheet SDS COA Handling Instructions Technical Support

PPI-GIT1/β-Pix interaction-IN-1 is a potent and orally active GIT1/β-Pix protein-protein interaction (PPI) inhibitor with a K_D value of 7.7 µM. PPI-GIT1/β-Pix interaction-IN-1 disrupts the GIT/PIX interaction can impact the activation of the downstream Rho GTPase Rac1 and Cdc42. PPI-GIT1/β-Pix interaction-IN-1 inhibits metastasis of gastric cancer.

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

PPI-GIT1/β-Pix interaction-IN-1 Chemical Structure

CAS No. : 2070916-70-8

Size	Stock	Quantity
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	Get quote
50 mg	Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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Biological Activity
Purity & Documentation
References
Customer Review

Description

In Vitro

PPI-GIT1/β-Pix interaction-IN-1 (compound 14-5-18; 0-50 μM) inhibits the interaction between GIT1 and β-Pix in living cells^[1].
PPI-GIT1/β-Pix interaction-IN-1 (0-50 μM; 24 h; MGC803 cells and MKN45 cells) inhibits gastric cancer cell invasion in a dose-dependent manner and disrupts the GIT/PIX interaction can impact the activation of the downstream Rho GTPase Rac1 and Cdc42^[1].

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

Western Blot Analysis^[1]

Cell Line:	MGC803 cells and MKN45 cells
Concentration:	0, 5, 20, and 50 μM
Incubation Time:	24 hours
Result:	Suppressed the expression of GTP-Rac1 and GTP-Cdc42 in a dose-dependent manner.

In Vivo

PPI-GIT1/β-Pix interaction-IN-1 (compound 14-5-18; 10 and 30 mg/kg; i.g.; 24 h) inhibits gastric cancer cell invasion in female nude mice with MGC803 xenografts^[1].

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

Animal Model:	Female nude mice with MGC803 xenografts (Four-week-old)^[1]
Dosage:	10 and 30 mg/kg
Administration:	oral gavage, daily, for 18 days
Result:	Reduced the luminescence intensity in the lungs in a dose-dependent manner.

Molecular Weight

391.42

Formula

C₂₃H₂₁NO₅

CAS No.

2070916-70-8

Appearance

Solid

Color

White to light brown

SMILES

O=C([C@@H]1[C@@H](C(OCC)=O)[C@]2(C(N(C)C3=C2C=CC=C3)=O)[C@H]/4C1)C4=C\C5=COC=C5

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 : 100 mg/mL (255.48 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	2.5548 mL	12.7740 mL	25.5480 mL
5 mM	0.5110 mL	2.5548 mL	5.1096 mL
10 mM	0.2555 mL	1.2774 mL	2.5548 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.39 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(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:

DMSO +

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

Purity: 99.01%

Select Batch:

Data Sheet (279 KB) SDS (252 KB)

COA (258 KB) HNMR (133 KB) RP-HPLC (304 KB) LCMS (98 KB)

Handling Instructions (2659 KB)

References

[1]. Gu J, et, al. Construction of a synthetic methodology-based library and its application in identifying a GIT/PIX protein-protein interaction inhibitor. Nat Commun. 2022 Nov 23;13(1):7176. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.5548 mL	12.7740 mL	25.5480 mL	63.8700 mL
	5 mM	0.5110 mL	2.5548 mL	5.1096 mL	12.7740 mL
	10 mM	0.2555 mL	1.2774 mL	2.5548 mL	6.3870 mL
	15 mM	0.1703 mL	0.8516 mL	1.7032 mL	4.2580 mL
	20 mM	0.1277 mL	0.6387 mL	1.2774 mL	3.1935 mL
	25 mM	0.1022 mL	0.5110 mL	1.0219 mL	2.5548 mL
	30 mM	0.0852 mL	0.4258 mL	0.8516 mL	2.1290 mL
	40 mM	0.0639 mL	0.3194 mL	0.6387 mL	1.5968 mL
	50 mM	0.0511 mL	0.2555 mL	0.5110 mL	1.2774 mL
	60 mM	0.0426 mL	0.2129 mL	0.4258 mL	1.0645 mL
	80 mM	0.0319 mL	0.1597 mL	0.3194 mL	0.7984 mL
	100 mM	0.0255 mL	0.1277 mL	0.2555 mL	0.6387 mL