SJB3-019A是一种新颖的、有效的USP1抑制剂，对K562细胞USP1的IC₅₀为0.0781μM。
Cas No.:2070015-29-9
Sample solution is provided at 25 µL, 10mM.
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SJB3-019A is a novel and potent USP1 inhibitor, exhibiting an IC₅₀ value of 0.0781μM in K562 cells[1-2]. SJB-019A can be used in the study of leukemia and related diseases[3-4].
In vitro, MM.1S multiple myeloma cells were treated with SJB3-019A (0.1–1μM) for 24 hours. SJB3-019A significantly induced the activation of caspase-3/8/9 and the cleavage of PARP, inhibited the DNA repair pathway by increasing the ubiquitination levels of FANCD2/FANCI/PCNA, and simultaneously downregulated the expression of the ID protein family to promote cell differentiation[5]. B-cell acute lymphoblastic leukemia cells (CCRF-SB, Sup-B15, and KOPN-8) were treated with SJB3-019A (0.2–0.6μM) for 24 hours. SJB3-019A significantly induced G2/M phase arrest and apoptosis via the mitochondrial pathway, and reduced AKT phosphorylation levels by inhibiting the USP1-ID1 axis[6].
In vivo, nude mice and C57BL/6 mice bearing MHCC-97H cell xenografts or orthotopic liver tumors were administered daily intraperitoneal injections of SJB3-019A (0.5mg/kg) in combination with Doxorubicin (1mg/kg) for 2 weeks. SJB3-019A significantly enhanced the tumor suppression induced by Doxorubicin[7].
References:
[1] Tan L, Shan H, Han C, et al. Discovery of Potent OTUB1/USP8 Dual Inhibitors Targeting Proteostasis in Non-Small-Cell Lung Cancer. J Med Chem. 2022 Oct 27;65(20):13645-13659.
[2] Kong T, Laranjeira ABA, Letson CT, et al. RSK1 dependency in FLT3-ITD acute myeloid leukemia. Blood Cancer J. 2024 Nov 26;14(1):207.
[3] Ishikawa C, Mori N. Role of Ubiquitin-specific Protease 1 in the Pathogenesis and Treatment of Adult T-Cell Leukemia. Anticancer Res. 2025 Nov;45(11):4827-4840.
[4] Takahashi H, Yamanaka S, Kuwada S, et al. A Human DUB Protein Array for Clarification of Linkage Specificity of Polyubiquitin Chain and Application to Evaluation of Its Inhibitors. Biomedicines. 2020 Jun 4;8(6):152.
[5] Das DS, Das A, Ray A, et al. Blockade of Deubiquitylating Enzyme USP1 Inhibits DNA Repair and Triggers Apoptosis in Multiple Myeloma Cells. Clin Cancer Res. 2017 Aug 1;23(15):4280-4289.
[6] Kuang X, Xiong J, Lu T, et al. Inhibition of USP1 induces apoptosis via ID1/AKT pathway in B-cell acute lymphoblastic leukemia cells. Int J Med Sci. 2021 Jan 1;18(1):245-255.
[7] Lu Z, Zhang Z, Yang M, et al. Ubiquitin-specific protease 1 inhibition sensitizes hepatocellular carcinoma cells to doxorubicin by ubiquitinated proliferating cell nuclear antigen-mediated attenuation of stemness. Anticancer Drugs. 2022 Aug 1;33(7):622-631.
SJB3-019A是一种新颖的、有效的USP1抑制剂，对K562细胞USP1的IC₅₀为0.0781μM[1-2]。SJB3-019A可用于白血病等相关疾病的研究[3-4]。
在体外，SJB3-019A（0.1–1μM）处理多发性骨髓瘤细胞MM.1S 24小时，SJB3-019A显著诱导caspase-3/8/9激活和PARP裂解，并通过增加FANCD2/FANCI/PCNA泛素化水平抑制DNA修复通路，同时下调ID蛋白家族表达促进细胞分化[5]。SJB3-019A（0.2–0.6μM）处理B细胞急性淋巴细胞白血病细胞（CCRF-SB、Sup-B15和KOPN-8）24小时，SJB3-019A显著诱导G2/M期阻滞和线粒体途径凋亡，并通过抑制USP1-ID1轴降低AKT磷酸化水平[6]。
在体内，SJB3-019A（0.5mg/kg）联合Doxorubicin（1mg/kg）每日一次腹腔注射，用于处理MHCC-97H细胞异种移植瘤或原位肝肿瘤模型的裸鼠及C57BL/6小鼠2周。SJB3-019A显著增强了Doxorubicin诱导的肿瘤抑制[7]。
| Cell experiment [1]: | |
Cell lines | CCRF-SB, Sup-B15, and KOPN-8 cells (human B-cell acute lymphoblastic leukemia lines) |
Preparation Method | Cells were cultured in complete medium with 10% fetal bovine serum at 37°C, 5% CO₂. Cells were treated with SJB3-019A at concentrations of 0.2–0.6μM for 24 hours. |
Reaction Conditions | 0.2–0.6μM; 24h. |
Applications | SJB3-019A significantly suppressed cell viability in a dose-dependent manner and induced apoptosis. SJB3-019A triggered G2/M phase cell cycle arrest. Mechanistically, SJB3-019A downregulated USP1 expression, leading to reduced ID1 protein levels and inhibition of AKT phosphorylation (p-AKT), thereby activating the ID1/AKT apoptotic pathway. |
| Animal experiment [2]: | |
Animal models | 6-week-old male nude mice with MHCC-97H cell-derived subcutaneous xenografts and C57BL/6 mice with orthotopic liver tumors |
Preparation Method | Mice were intraperitoneally injected with SJB3-019A (0.5mg/kg/day) alone or in combination with Doxorubicin (1mg/kg/day) for 2 weeks. |
Dosage form | 0.5mg/kg/day; 14-day treatment. |
Applications | SJB3-019A significantly enhanced Dox-induced tumor growth inhibition in both subcutaneous xenograft and orthotopic liver tumor models, with combined treatment showing superior efficacy compared to monotherapy. |
References: | |
| Cas No. | 2070015-29-9 | SDF | |
| 化学名 | 2-(pyridin-3-yl)naphtho[2,3-d]oxazole-4,9-dione | ||
| Canonical SMILES | O=C(C1=C2OC(C3=CN=CC=C3)=N1)C4=CC=CC=C4C2=O | ||
| 分子式 | C16H8N2O3 | 分子量 | 276.25 |
| 溶解度 | ≥ 10.85mg/mL in DMSO with gentle warming | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.6199 mL | 18.0995 mL | 36.1991 mL |
| 5 mM | 724 μL | 3.6199 mL | 7.2398 mL |
| 10 mM | 362 μL | 1.81 mL | 3.6199 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
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计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
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- Purity: >97.00% Appearance: A solid
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