2. PI3K/Akt/mTOR
  3. PIN1
  4. Sulfopin

Sulfopin (PIN1-3) is a highly selective covalent inhibitor of Pin1 with an apparent Ki of 17 nM. Sulfopin blocks Myc-driven tumors in vivo. The peptidyl-prolyl isomerase, Pin1, is exploited in cancer to activate oncogenes and inactivate tumor suppressors.

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Sulfopin Chemical Structure

Sulfopin Chemical Structure

CAS No. : 2451481-08-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 105 In-stock
Solution
10 mM * 1 mL in DMSO USD 105 In-stock
Solid
5 mg USD 95 In-stock
10 mg USD 155 In-stock
25 mg USD 315 In-stock
50 mg USD 504 In-stock
100 mg USD 805 In-stock
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Based on 2 publication(s) in Google Scholar

Sulfopin Related Antibodies

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Description

Sulfopin (PIN1-3) is a highly selective covalent inhibitor of Pin1 with an apparent Ki of 17 nM. Sulfopin blocks Myc-driven tumors in vivo. The peptidyl-prolyl isomerase, Pin1, is exploited in cancer to activate oncogenes and inactivate tumor suppressors[1].

In Vitro

MDA-MB-468 cells show the most pronounced sensitivity to Sulfopin (1, 2.5 μM; 4-8 days)[1].
Sulfopin (2 μM, HEK293 cells; 48 hours) downregulates Myc transcription[1].
Sulfopin (1, 2.5 μM; PATU-8988T cells; 4 days) shows a small but significant reduction in the number of synthesis (S)-phase cells and a corresponding increase of growth 1 (G1)-phase cells[1].

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

Sulfopin Related Antibodies

Cell Proliferation Assay[1]

Cell Line: Kuramochi, MDA-MB-468, NGP, NBL-S, MDA-MB-468 cells
Concentration: 1, 2.5 μM
Incubation Time: 4,6, 8 days
Result: Showed variation in antiproliferative effects across cancer cell lines Kuramochi, MDA-MB-468, NGP and NBL-S, with the most pronounced sensitivity observed in MDA-MB-468 cells.
In Vivo

Sulfopin (40 mg/kg; p.o.; QD/BID for 7 days) regresses neuroblastoma in mice[1].
Sulfopin (20-40 mg/kg; i.p.; daily for 27 days) inhibits pancreatic cancer progression in mice[1].
Sulfopin (25-100 μM) blocks neuroblastoma in zebrafish[1].

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

Animal Model: Transgenic Th-MYCN mice[1]
Dosage: 40 mg/kg
Administration: Once a day (QD) or twice a day (BID) for 7 days
Result: Sulfopin-treated QD mice showed a significant average increase in survival of 10 days, while Sulfopin-treated BID mice showed an even more pronounced average increase of 28 days.
Molecular Weight

281.80

Formula

C11H20ClNO3S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N(CC(C)(C)C)C(CC1)CS1(=O)=O)CCl
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 (354.86 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 4.35 mg/mL (15.44 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.5486 mL 17.7431 mL 35.4862 mL
5 mM 0.7097 mL 3.5486 mL 7.0972 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.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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C2

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Volume (final)

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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (8.87 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (8.87 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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: 99.69%

SDS (555 KB)

COA (253 KB) HNMR (250 KB) LCMS (257 KB)

Handling Instructions (2659 KB)
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
H2O / DMSO 1 mM 3.5486 mL 17.7431 mL 35.4862 mL 88.7154 mL
5 mM 0.7097 mL 3.5486 mL 7.0972 mL 17.7431 mL
10 mM 0.3549 mL 1.7743 mL 3.5486 mL 8.8715 mL
15 mM 0.2366 mL 1.1829 mL 2.3657 mL 5.9144 mL
DMSO 20 mM 0.1774 mL 0.8872 mL 1.7743 mL 4.4358 mL
25 mM 0.1419 mL 0.7097 mL 1.4194 mL 3.5486 mL
30 mM 0.1183 mL 0.5914 mL 1.1829 mL 2.9572 mL
40 mM 0.0887 mL 0.4436 mL 0.8872 mL 2.2179 mL
50 mM 0.0710 mL 0.3549 mL 0.7097 mL 1.7743 mL
60 mM 0.0591 mL 0.2957 mL 0.5914 mL 1.4786 mL
80 mM 0.0444 mL 0.2218 mL 0.4436 mL 1.1089 mL
100 mM 0.0355 mL 0.1774 mL 0.3549 mL 0.8872 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Sulfopin 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:

Sulfopin2451481-08-4PIN1-3PIN1peptidylprolyl cis/trans isomerase, NIMA-interacting 1MDA-MB-468cellstumorsantiproliferativeHEK293neuroblastomapancreaticcancerInhibitorinhibitorinhibit

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