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Pitstop 2 Clathrin Inhibitor

Name: Pitstop 2
Brand: Selleck Chemicals
SKU: S9670
Availability: InStock
Rating: 5 (9 reviews)

Cat.No.S9670

Pitstop 2 is an inhibitor of the interaction of amphiphysin with the amino terminal domain of clathrin that inhibits both clathrin-dependent endocytosis (CDE) and clathrin independent endocytosis (CIE).

Chemical Structure

Molecular Weight: 473.36

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Quality Control

Batch: S967001 DMSO]95 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 98.92%

Cited in Nature Medicine for its top-tier quality
COA
NMR
HPLC
SDS
Datasheet

98.92

Related Targets	Bcl-2 Caspase K-Ras PD-1/PD-L1 Ferroptosis p53 Synthetic Lethality STAT TNF-alpha Ras
Other Apoptosis related Inhibitors	Importazole Genipin Plumbagin 6-Gingerol Crocin Colcemid Euphorbia factor L3 Sophoridine Pomolic acid Flavone

Solubility

In vitro
Batch:

DMSO : 95 mg/mL (200.69 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.750mg/ml (10.03mM)	Taking the 1 mL working solution as an example, add 50 μL of 95 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.800mg/ml (1.69mM)	Taking the 1 mL working solution as an example, add 50 μL of 16 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	473.36	Formula	C₂₀H₁₃BrN₂O₃S₂	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1332879-52-3	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	BrC1=CC=C(C=C1)\C=C2/SC(=NC2=O)N[S](=O)(=O)C3=CC=CC4=C3C=CC=C4

Mechanism of Action

Targets/IC₅₀/Ki	CIE
In vitro	Pitstop 2 is an inhibitor of the interaction of amphiphysin with the amino terminal domain of clathrin and inhibits clathrin-dependent endocytosis (CDE) and clathrin independent endocytosis (CIE) in cells. The effects of pitstop 2 are not restricted to inhibition of clathrin since knockdown of clathrin fails to rescue the inhibition of endocytosis of CIE proteins by the drug. Thus pitstop 2 has additional cellular targets besides the amino terminal domain of clathrin and thus cannot be used to distinguish CIE from CDE.
References	[1] https://pubmed.ncbi.nlm.nih.gov/23029248/

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