2. PI3K/Akt/mTOR
  3. PIN1
  4. KPT-6566

KPT-6566 is a selective and covalent prolyl isomerase PIN1 inhibitor, covalently binds to the catalytic site of PIN1, selectively inhibits and degrades PIN1. KPT-6566 shows an IC50 value of 640 nM and a Ki value of 625.2 nM for PIN1 PPIase domain. KPT-6566 can be used for the research of cancer.

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

KPT-6566 Chemical Structure

KPT-6566 Chemical Structure

CAS No. : 881487-77-0

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 351 In-stock
Solution
10 mM * 1 mL in DMSO USD 351 In-stock
Solid
1 mg USD 120 In-stock
5 mg USD 360 In-stock
10 mg USD 550 In-stock
25 mg USD 1100 In-stock
50 mg USD 1760 In-stock
100 mg USD 2820 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

KPT-6566 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

KPT-6566 is a selective and covalent prolyl isomerase PIN1 inhibitor, covalently binds to the catalytic site of PIN1, selectively inhibits and degrades PIN1. KPT-6566 shows an IC50 value of 640 nM and a Ki value of 625.2 nM for PIN1 PPIase domain. KPT-6566 can be used for the research of cancer[1].

IC50 & Target

IC50: 640 nM (PIN1 PPIase)[1]
Ki: 625.2 nM (PIN1 PPIase)[1]
In Vitro

KPT-6566 (1-5 μM; 0-8 d) inhibits WT fibroblasts proliferation[1].
KPT-6566 (0-10 μM; 48 h) inhibits normal breast epithelial cells and cancer cells viability via a PIN1-dependent manner[1].
KPT-6566 (0-10 μM; 48 h) affects hyperphosphorylated pRB level, Cyclin D1 and PIN1 concentration[1].
KPT-6566 (2.5-5 μM; 48 h) inhibits the mut-p53, NOTCH1 and NRF2 pathways[1].
KPT-6566 (0-5 μM; 48 h) induces DNA damage via a PIN1-dependent way[1].

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

KPT-6566 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: Immortalized fibroblasts derived from WT and Pin1 KO mouse embryos
Concentration: 1 and 5 μM
Incubation Time: 0-8 days
Result: Dose-dependently inhibited proliferation of WT fibroblasts, while showed no effect on Pin1 KO fibroblasts.

Cell Viability Assay[1]

Cell Line: MCF10A, HMEC, HeLa, LNCaP, SKOV-3, PANC-1, PC-3, MDA-MB-468 and MDA-MB-231 cells
Concentration: 0-10 μM
Incubation Time: 48 hours
Result: Inhibited normal breast epithelial cells and cancer cells viability even at a low concentration and increased the concentration of PIN1 in MDA-MB-468, SKOV-3, PC-3, LNCaP and PANC-1.

Western Blot Analysis[1]

Cell Line: Immortalized fibroblasts derived from WT and Pin1 KO mouse embryos and PIN1 KO MDA-MB-231 cells
Concentration: 0-10 μM
Incubation Time: 48 hours
Result: Decreased hyperphosphorylated pRB and Cyclin D1 levels, dose- and time-dependently promoted degradation of PIN1 .

Western Blot Analysis[1]

Cell Line: MDA-MB-231, MCF10A, MDA-MB-468 and MDA-MB-231 cells
Concentration: 0, 2.5 and 5 μM
Incubation Time: 48 hours
Result: Dose-dependently increased H2AX phosphorylation and caused H2AX phosphorylation in MCF10A, MDA-MB-468 and MDA-MB-231 cell lines. Increased H2AX phosphorylation while other inhibitors such as ATRA, PiB and Juglone disabled to induce H2AX phosphorylation at same concentration. Achieved DNA damage through formation of DNA adducts.

RT-PCR[1]

Cell Line: MDA-MB-231 cells
Concentration: 2.5 and 5 μM
Incubation Time: 48 hours
Result: Dose-dependently inhibitd the activation of mut-p53 and NOTCH1 pathways which are controlled by PIN1. Inhibitd the expression of cFOS HO1, NQO1, TXNRD1 and DNAJAB, and induced cellular responses to oxidative stress.
In Vivo

KPT-6566 (5 mg/kg; i.p. once a day for 26 days) shows no toxicity to mice[1].

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

Animal Model: 6-week-old female mice with 1 million of MDA-MB-231Luc6 cells injection[1]
Dosage: 5 mg/kg
Administration: Intraperitoneal injection; 5 mg/kg once a day; for 26 days
Result: Exibited no sign of local or systemic and organ toxicity by post mortem morphologic analyses.
Molecular Weight

443.54

Formula

C22H21NO5S2
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

O=C(O)CSC(C1=O)=C/C(C2=C1C=CC=C2)=N\S(=O)(C3=CC=C(C(C)(C)C)C=C3)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 19.23 mg/mL (43.36 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 2.2546 mL 11.2729 mL 22.5459 mL
5 mM 0.4509 mL 2.2546 mL 4.5092 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 (protect from light, stored under nitrogen). 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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
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: 1.92 mg/mL (4.33 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 1.92 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (19.2 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: ≥ 1 mg/mL (2.25 mM); Clear solution

    This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

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: ≥98.0%

COA (258 KB) HNMR (267 KB) MS (86 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 (protect from light, stored under nitrogen). 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 2.2546 mL 11.2729 mL 22.5459 mL 56.3647 mL
5 mM 0.4509 mL 2.2546 mL 4.5092 mL 11.2729 mL
10 mM 0.2255 mL 1.1273 mL 2.2546 mL 5.6365 mL
15 mM 0.1503 mL 0.7515 mL 1.5031 mL 3.7576 mL
20 mM 0.1127 mL 0.5636 mL 1.1273 mL 2.8182 mL
25 mM 0.0902 mL 0.4509 mL 0.9018 mL 2.2546 mL
30 mM 0.0752 mL 0.3758 mL 0.7515 mL 1.8788 mL
40 mM 0.0564 mL 0.2818 mL 0.5636 mL 1.4091 mL
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KPT-6566 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:

KPT-6566881487-77-0KPT6566KPT 6566PIN1peptidylprolyl cis/trans isomerase, NIMA-interacting 1breast epithelialanti- proliferationCyclin D1MDA-MB-231 cellROSDNA damageInhibitorinhibitorinhibit

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