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KPT-6566 

Cat. No.: HY-123847 Purity: ≥98.0%
Handling Instructions

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
Solution
10 mM * 1 mL in DMSO USD 351 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 351 In-stock
Estimated Time of Arrival: December 31
Solid
1 mg USD 120 In-stock
Estimated Time of Arrival: December 31
5 mg USD 360 In-stock
Estimated Time of Arrival: December 31
10 mg USD 550 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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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].

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

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].

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.
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)

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
10 mM 0.2255 mL 1.1273 mL 2.2546 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: ≥98.0%

References
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Product Name:
KPT-6566
Cat. No.:
HY-123847
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