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PIN1 inhibitor API-1

SKU: orb1217737

Description

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

Research Area

Pharmacology & Drug Discovery

Images & Validation

Key Properties

CAS Number680622-70-2
MW366.3
Purity>98% (HPLC)
FormulaC15H13F3N6O2
SMILESC1=CC(=CC=C1CNC(=O)C(F)(F)F)COC2=NC(=NC3=C2NC=N3)N
TargetPin1
SolubilityDMSO:250 mg/mL (682.50 mM; Need ultrasonic)

Bioactivity

In Vivo
PIN1 inhibitor API-1 suppresses tumor growth in mice by up-regulating mature miRNA biogenesis.
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).

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

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    680622-70-2

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    C15H13F3N6O2

    1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg, 200 mg, 1 ml x 10 mM (in DMSO), 500 mg
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PIN1 inhibitor API-1 (orb1217737)

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Available Sizes

Select a size below

500 mg
5 mg
¥ 3,640.00
10 mg
¥ 6,630.00
25 mg
¥ 9,230.00
50 mg
¥ 13,260.00
100 mg
¥ 16,900.00
200 mg
¥ 24,570.00