GLPBio

PIN1 inhibitor API-1

Catalog No.: GC38036Purity:>98.00%
COASDSData Sheet
PIN1 阻害剤 API-1 は、特定の Pin1 (ペプチジル-プロリル シス-トランス イソメラーゼ NIMA 相互作用 1) 阻害剤 (API-1) であり、IC50 は 72.3 nM です。 PIN1 阻害剤 API-1 は、Pin1 ペプチジル-プロリルイソメラーゼ (PPIase) ドメインに直接的かつ特異的に結合し、Pin1 cis-trans 異性化活性を強力に阻害します。 PIN1 阻害剤 API-1 は、pXPO5 の活性立体構造を保持し、pXPO5 が pre-miRNA を核から細胞質に輸送する能力を回復させ、抗がん miRNA の生合成をアップレギュレートして、in vitro および in vivo での肝細胞がんの発生を抑制します。

製品は研究用途にのみ使用できます。人体には使用できません。患者への販売は行っておりません。

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
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引用文献 (Citations)

現在、この製品の引用文献はありません。以下はGlpBio製品を引用した代表的な文献です。
  • Nature cover
    Nature
    641, 529–536 (2025)
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    Nature
    628, 630–638 (2024)
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    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)
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    Cell Research
    35, 97–116 (2025)
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    Cell Research
    34, 683–706 (2024)
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    Cell Research
    33, 273–287 (2023)
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    Cell Research
    33, 546–561 (2023)
  • Cell Research cover
    Cell Research
    33, 904–922 (2023)
  • Cell Research cover
    Cell Research
    31, 1291–1307 (2021)

製品説明 (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.

実験プロトコル (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.

製品資料 (Product Documents)

Purity:>98.00%Appearance:A solid
COASDSData Sheet

化学的性質 (Chemical Properties)

CAS番号
680622-70-2
SMILES
O=C(NCC1=CC=C(COC2=C3NC=NC3N=C(N)N2)C=C1)C(F)(F)F
分子式
C15H15F3N6O2
分子量
368.31
溶解性
DMSO: 250 mg/mL (682.50 mM)
保存条件
Store at -20°C
一般的な注意事項
製品の溶解性データに基づいて適切な溶媒を選択してください。調製後は、凍結融解の繰り返しを避けるため、ストック溶液を小分けしてください。
ストック溶液は、-80°Cで保存する場合は6か月以内、-20°Cで保存する場合は1か月以内に使用してください。
溶解性を高めるには、チューブを37°Cに温め、適切な時間超音波処理してください。
配送条件
評価用サンプルは保冷剤とともに発送します。その他の容量は室温で発送し、ご要望に応じて保冷剤を同梱します。

計算ツール (Calculators)モル濃度 / 希釈 / 分子量 / 単位変換 / in vivo製剤 / 溶解度

g/mol

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