GLPBio

PIN1 inhibitor API-1

Catalog No.: GC38036Purity:>98.00%
COASDSData Sheet
El inhibidor de PIN1 API-1 es un inhibidor especÍfico de Pin1 (peptidil-prolil cis-trans isomerasa NIMA-interacting 1) (API-1) con una IC50 de 72,3 nM. El inhibidor de PIN1 API-1 se une directa y especÍficamente al dominio Pin1 peptidil-prolil isomerasa (PPIasa) e inhibe potentemente la actividad isomerizante cis-trans de Pin1. El inhibidor de PIN1 API-1 retiene la conformaciÓn activa de pXPO5 y restaura la capacidad de pXPO5 para transportar pre-miARN desde el nÚcleo al citoplasma, regulando asÍ la biogénesis de miARN contra el cÁncer para suprimir el desarrollo de carcinoma hepatocelular tanto in vitro como in vivo.

Los productos son exclusivamente para uso en investigación. No aptos para uso humano. No vendemos a pacientes.

PIN1 inhibitor API-1
Cas No.: 680622-70-2
10mM (in 1mL DMSO)In Stock
$131.00
1
1mgIn Stock
$40.00
1
5mgIn Stock
$119.00
1
10mgIn Stock
$223.00
1
25mgIn Stock
$320.00
1
50mgIn Stock
$462.00
1
100mgIn Stock
$610.00
1
200mgIn Stock
$825.00
1
Tel: (909) 407-4943 / (909) 689-7124Email: sales@glpbio.com

Citas (Citations)

Actualmente no hay citas disponibles para este producto. A continuación se muestran publicaciones seleccionadas que citan productos GlpBio.
  • Nature cover
    Nature
    641, 529–536 (2025)
  • Nature cover
    Nature
    628, 630–638 (2024)
  • Nature cover
    Nature
    632, 686–694 (2024)
  • Nature cover
    Nature
    618, 1017–1023 (2023)
  • Nature cover
    Nature
    610, 366–372 (2022)
  • Cell cover
    Cell
    187(9):2288-2304 (2024)
  • Cell cover
    Cell
    183(7):1867-1883 (2020)
  • Science cover
    Science
    388(6745) (2025)
  • Science cover
    Science
    387(6739) (2025)
  • Science cover
    Science
    387(6734) (2025)
  • Cell Research cover
    Cell Research
    35, 97–116 (2025)
  • Cell Research cover
    Cell Research
    34, 683–706 (2024)
  • Cell Research cover
    Cell Research
    33, 273–287 (2023)
  • Cell Research cover
    Cell Research
    33, 546–561 (2023)
  • Cell Research cover
    Cell Research
    33, 904–922 (2023)
  • Cell Research cover
    Cell Research
    31, 1291–1307 (2021)

Descripción (Description)

PIN1 inhibitor API-1 is a specific Pin1 (peptidyl-prolyl cis-trans isomerase NIMA-interacting 1) inhibitor with an IC50 of 72.3nM. PIN1 inhibitor API-1 targets the Pin1 peptidyl-prolyl isomerase domain and inhibits its cis-trans isomerase activity[1].

In vitro, PIN1 inhibitor API-1 decreased SK-Hep-1 cell proliferation with IC50 0.68μM[1]. PIN1 inhibitor API-1(1μM; 24-48h) significantly increased the expression of mature miRNAs including miR-122, let-7a, miR-29b and miR-146a[1]. PIN1 inhibitor API-1 inhibited the viability of BRAF-mutant thyroid cancer cell lines 8505C, BCPAP and SW1736, with IC50 values of 39.45±6.54μM, 49.97±7.73μM, and 44.70±6.86μM, respectively[2].

In vivo, treatment of PIN1 inhibitor API-1 (5mg/kg and 10mg/kg; i.v.; q2d; 16 days) suppressed tumor growth in SK-Hep-1- and Hep3B-derived hepatocellular carcinoma xenograft mouse models[1].

References:
[1]. Pu, Wenchen, et al. "Targeting Pin1 by inhibitor API‐1 regulates microRNA biogenesis and suppresses hepatocellular carcinoma development." Hepatology 68.2 (2018): 547-560.
[2]. Dang, Hui, et al. "Pin1 inhibitor API-1 sensitizes BRAF-mutant thyroid cancers to BRAF inhibitors by attenuating HER3-mediated feedback activation of MAPK/ERK and PI3K/AKT pathways." International Journal of Biological Macromolecules 248 (2023): 125867.

Protocolo (Protocol)

Cell experiment [1]:

Cell lines

BRAF-mutant thyroid cancer cell lines 8505C, BCPAP and SW1736

Preparation Method

Cells (800–1500/well) were cultured in 96-well plates and then treated with PIN1 inhibitor API-1, at the indicated concentrations and times.

Reaction Conditions

0-2μM; 48h

Applications

PIN1 inhibitor API-1 inhibited the viability of BRAF-mutant thyroid cancer cell lines 8505C, BCPAP and SW1736, with IC50 values of 39.45±6.54μM, 49.97±7.73μM, and 44.70±6.86μM, respectively.
Animal experiment [2]:

Animal models

Hepatocellular carcinoma xenograft mouse model

Preparation Method

Hepatocellular carcinoma (HCC) cells (API-1, SK-Hep-1, Hep3B) were harvested during the exponential-growth phase and washed with serum-free medium, followed by resuspension in Matrigel at a concentration of 3×107/mL. Then, 100μL of cell suspension was injected into female BALB/c mice (5 weeks old) subcutaneously. After the tumor sizes reached 150-200mm3, all mice were randomized into two groups (six mice per group) and intravenously injected with PIN1 inhibitor API-1 (5 or 10mg/kg/2 days) or vehicle, which was prepared in normal saline solution with 5% dimethyl sulfoxide (DMSO). Tumor growth was recorded every 3 days.

Dosage form

5mg/kg and 10mg/kg; i.v.; q2d; 16 days

Applications

In xenograft mice, PIN1 inhibitor API-1 suppressed SK-Hep-1 and Hep3B tumor growth. But PIN1 inhibitor API-1 was not sensitive to SMMC-7721 tumors.

References:
[1]. Dang, Hui, et al. "Pin1 inhibitor API-1 sensitizes BRAF-mutant thyroid cancers to BRAF inhibitors by attenuating HER3-mediated feedback activation of MAPK/ERK and PI3K/AKT pathways." International Journal of Biological Macromolecules 248 (2023): 125867.
[2]. Pu, Wenchen, et al. "Targeting Pin1 by inhibitor API‐1 regulates microRNA biogenesis and suppresses hepatocellular carcinoma development." Hepatology 68.2 (2018): 547-560.

Documentos del producto (Product Documents)

Purity:>98.00%Appearance:A solid
COASDSData Sheet

Propiedades químicas (Chemical Properties)

N.º CAS
680622-70-2
SMILES
O=C(NCC1=CC=C(COC2=C3NC=NC3N=C(N)N2)C=C1)C(F)(F)F
Fórmula molecular
C15H15F3N6O2
Peso molecular
368.31
Solubilidad
DMSO: 250 mg/mL (682.50 mM)
Almacenamiento
Store at -20°C
Consejos generales
Seleccione un disolvente adecuado según los datos de solubilidad del producto. Una vez preparada, divida la solución madre en alícuotas para evitar ciclos repetidos de congelación y descongelación.
Utilice las soluciones madre en un plazo de 6 meses si se conservan a -80°C, o de 1 mes si se conservan a -20°C.
Para mejorar la solubilidad, caliente el tubo a 37°C y soníquelo durante un periodo adecuado.
Condiciones de envío
Las muestras de evaluación se envían con acumuladores de frío. Los demás tamaños se envían a temperatura ambiente o, previa solicitud, con acumuladores de frío.

Calculadoras (Calculators)Molaridad / Dilución / Peso molecular / Conversión de unidades / Formulación in vivo / Solubilidad

g/mol

Reviews

Review for PIN1 inhibitor API-1

Rating: 5
  • 5 Star100%
  • 4 Star0%
  • 3 Star0%
  • 2 Star0%
  • 1 Star0%