1. Epigenetics
  2. MicroRNA
  3. PIN1 inhibitor API-1

PIN1 inhibitor API-1 

Cat. No.: HY-116716 Purity: 97.03%
Handling Instructions

PIN1 inhibitor API-1 is a specific Pin1 (peptidyl-prolyl cis-trans isomerase NIMA-interacting 1) inhibitor (API-1) with an IC50 of 72.3 nM. PIN1 inhibitor API-1 directly and specifically binds to the Pin1 peptidyl-prolyl isomerase (PPIase) domain and potently inhibits Pin1 cis-trans isomerizing activity. PIN1 inhibitor API-1 retains the active conformation of pXPO5 and restores the ability of pXPO5 to transport pre-miRNAs from nucleus to cytoplasm, thus up-regulating the anticancer miRNA biogenesis to suppress both in vitro and in vivo hepatocellular carcinoma development.

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

PIN1 inhibitor API-1 Chemical Structure

PIN1 inhibitor API-1 Chemical Structure

CAS No. : 680622-70-2

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 201 In-stock
Estimated Time of Arrival: December 31
5 mg USD 250 In-stock
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10 mg USD 450 In-stock
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25 mg USD 900 In-stock
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50 mg USD 1600 In-stock
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100 mg USD 2800 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

PIN1 inhibitor API-1 is a specific Pin1 (peptidyl-prolyl cis-trans isomerase NIMA-interacting 1) inhibitor (API-1) with an IC50 of 72.3 nM. PIN1 inhibitor API-1 directly and specifically binds to the Pin1 peptidyl-prolyl isomerase (PPIase) domain and potently inhibits Pin1 cis-trans isomerizing activity. PIN1 inhibitor API-1 retains the active conformation of pXPO5 and restores the ability of pXPO5 to transport pre-miRNAs from nucleus to cytoplasm, thus up-regulating the anticancer miRNA biogenesis to suppress both in vitro and in vivo hepatocellular carcinoma development[1].

IC50 & Target

IC50: 72.3 nM (Pin1)[1]

In Vitro

PIN1 inhibitor API-1 obviously inhibits SK-Hep-1, SNU-423, and Hep3B cell proliferation with low IC50 values (IC50=0.683-4.16 μM)[1].

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

In Vivo

PIN1 inhibitor API-1 suppresses tumor growth in mice by up-regulating mature miRNA biogenesis[1].

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

Molecular Weight

366.30

Formula

C₁₅H₁₃F₃N₆O₂

CAS No.

680622-70-2

SMILES

O=C(NCC1=CC=C(COC2=C3NC=NC3=NC(N)=N2)C=C1)C(F)(F)F

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 : 250 mg/mL (682.50 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7300 mL 13.6500 mL 27.3000 mL
5 mM 0.5460 mL 2.7300 mL 5.4600 mL
10 mM 0.2730 mL 1.3650 mL 2.7300 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: ≥ 2.17 mg/mL (5.92 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.17 mg/mL (5.92 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.17 mg/mL (5.92 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 97.03%

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Keywords:

PIN1 inhibitor API-1MicroRNAmiRNAInhibitorinhibitorinhibit

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Product Name:
PIN1 inhibitor API-1
Cat. No.:
HY-116716
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