GLPBio

PIN1 inhibitor API-1

Catalog No.: GC38036Purity:>98.00%
COASDSData Sheet
PIN1 억제제 API-1은 IC50이 72.3nM인 특정 Pin1(펩티딜-프롤릴 시스-트랜스 이성질화효소 NIMA-상호작용 1) 억제제(API-1)입니다. PIN1 억제제 API-1은 Pin1 펩티딜-프롤릴 이성화효소(PPIase) 도메인에 직접 및 특이적으로 결합하여 Pin1 시스-트랜스 이성화 활성을 강력하게 억제합니다. PIN1 억제제 API-1은 pXPO5의 활성 형태를 유지하고 pXPO5가 pre-miRNA를 핵에서 세포질로 수송하는 능력을 복원하여 항암 miRNA 생합성을 상향 조절하여 시험관 내 및 생체 내 간세포 암종 발병을 모두 억제합니다.

제품은 연구용으로만 사용됩니다. 인체에 사용할 수 없으며 환자에게 판매하지 않습니다.

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

인용 문헌 (Citations)

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제품 설명 (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.

실험 프로토콜 (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.

제품 문서 (Product Documents)

Purity:>98.00%Appearance:A solid
COASDSData Sheet

화학적 특성 (Chemical Properties)

CAS 번호
680622-70-2
SMILES
O=C(NCC1=CC=C(COC2=C3NC=NC3N=C(N)N2)C=C1)C(F)(F)F
분자식
C15H15F3N6O2
분자량
368.31
용해도
DMSO: 250 mg/mL (682.50 mM)
보관
Store at -20°C
일반 주의사항
제품의 용해도 데이터에 따라 적절한 용매를 선택하십시오. 조제 후에는 반복적인 동결·해동을 피할 수 있도록 저장 용액을 소분하십시오.
저장 용액은 -80°C 보관 시 6개월 이내, -20°C 보관 시 1개월 이내에 사용하십시오.
용해도를 높이려면 튜브를 37°C로 데운 뒤 적절한 시간 동안 초음파 처리하십시오.
배송 조건
평가용 샘플은 아이스팩과 함께 배송됩니다. 그 외 용량은 실온 배송되며, 요청 시 아이스팩과 함께 배송할 수 있습니다.

계산 도구 (Calculators)몰 농도 / 희석 / 분자량 / 단위 변환 / 생체 내 제형 / 용해도

g/mol

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