VLX1570
Based on 2 publication(s) in Google Scholar
VLX1570 is a competitive inhibitor of proteasome deubiquitinases (DUBs) with an IC50 of approximate 10 μM.
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- 純度 : 99.95%
- CAS 番号: 1431280-51-1
- 分子式: C23H17F2N3O6
- 分子量:469.39
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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b-AP15UCHL5/Usp14 Inhibitor
MedChemExpress（MCE）の使用を引用している文献 VLX1570
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生物活性
製品説明
IC50 & Target
IC50: appr 10 μM (Deubiquitinase)[2]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | EC50 |
0.58 μM
Compound: VLX1570
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Cytotoxicity in human HCT116 cells assessed as reduction in cell viability incubated for 72 hrs by FMCA analysis
Cytotoxicity in human HCT116 cells assessed as reduction in cell viability incubated for 72 hrs by FMCA analysis
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[PMID: 31682427] |
| KMS-11 | EC50 |
43 nM
Compound: VLX1570
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Cytotoxicity in human KMS11 cells assessed as reduction in cell viability incubated for 72 hrs Cell-titer Glo reagent based assay
Cytotoxicity in human KMS11 cells assessed as reduction in cell viability incubated for 72 hrs Cell-titer Glo reagent based assay
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[PMID: 32109059] |
| U2OS | EC50 |
98 nM
Compound: VLX1570
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Cytotoxicity in human U2OS cells assessed as reduction in cell viability incubated for 72 hrs Cell-titer Glo reagent based assay
Cytotoxicity in human U2OS cells assessed as reduction in cell viability incubated for 72 hrs Cell-titer Glo reagent based assay
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[PMID: 32109059] |
体外実験
VLX1570 inhibits USP14 and UCHL5 activity of 19S regulatory particles, and the inhibition of USP14 is more pronounced. VLX1570 (1 μM) shows inhibitory activity against USP14 in KMS-11 myeloma cells. VLX1570 exhibits an IC50 of 0.58 μM on HCT116 cells[1]. VLX1570 binds to recombinant USP14 with Kd of 1.5-18?μM using two different sources of recombinant protein, and the Kd for recombinant UCHL5 is higher (14-18?μM) compared to that of USP14. VLX1570 has potent antiproliferative activities on multiple myeloma cells, with IC50s of 43?±?2 nM, 74?±?2 nM, 126?±?3 nM, and 191?±?1 nM for KMS-11, RPMI8226, OPM-2, and OPM-2-BZR cells, respectively[2]. VLX1570 suppresses the viability of BCWM.1 cells, with an EC50 of 20.22?nM. VLX1570 (100, 250, 500 nM) induces significant apoptosis by 12?h in a dose-dependent manner in all Waldenstrom macroglobulinemia (WM) cell lines tested, including BCWM.1/IR (IR) and BCWM.1/BR (BR) subclones. VLX1570 (100, 250, 500 nM) also causes ER stress machinery and mitochondrial damage in WM cells. VLX1570 (250?nM) downregulates BCR-signalosome components and their end effectors, as well as CXCR4 expression in WM cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1431280-51-1
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性状 Solid
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分子量 469.39
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分子式 C23H17F2N3O6
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Color White to yellow
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SMILES
O=C1/C(CN(C(C=C)=O)CC/C1=C\C2=CC=C(F)C([N+]([O-])=O)=C2)=C/C3=CC=C(F)C([N+]([O-])=O)=C3
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Cell Death Dis
TRIB2 modulates proteasome function to reduce ubiquitin stability and protect liver cancer cells against oxidative stress. [Abstract]2021 Jan 7;12(1):42. PMID: 33414446 -
Mol Cancer Ther
Targeting the Proteasome-Associated Deubiquitinating Enzyme USP14 Impairs Melanoma Cell Survival and Overcomes Resistance to MAPK-Targeting Therapies. [Abstract]2018 Jul;17(7):1416-1429. PMID: 29703842
VLX1570 purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2018 Jul;17(7):1416-1429. [Abstract]
VLX1570 blocks USP14, but not UCHL5, activity in melanoma.
溶剤 & 溶解度
体外:
DMSO : ≥ 32 mg/mL (68.17 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (283 KB)
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SDS (393 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Wang X, et al. Synthesis and evaluation of derivatives of the proteasome deubiquitinase inhibitor b-AP15. Chem Biol Drug Des. 2015 Nov;86(5):1036-48. [Content Brief]
[2]. Wang X, et al. The proteasome deubiquitinase inhibitor VLX1570 shows selectivity for ubiquitin-specific protease-14 and induces apoptosis of multiple myeloma cells. Sci Rep. 2016 Jun 6;6:26979. [Content Brief]
[3]. Paulus A, et al. Coinhibition of the deubiquitinating enzymes, USP14 and UCHL5, with VLX1570 is lethal to ibrutinib- or bortezomib-resistant Waldenstrom macroglobulinemia tumor cells. Blood Cancer J. 2016 Nov 4;6(11):e492. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1304 mL | 10.6521 mL | 21.3042 mL | 53.2606 mL |
| 5 mM | 0.4261 mL | 2.1304 mL | 4.2608 mL | 10.6521 mL | |
| 10 mM | 0.2130 mL | 1.0652 mL | 2.1304 mL | 5.3261 mL | |
| 15 mM | 0.1420 mL | 0.7101 mL | 1.4203 mL | 3.5507 mL | |
| 20 mM | 0.1065 mL | 0.5326 mL | 1.0652 mL | 2.6630 mL | |
| 25 mM | 0.0852 mL | 0.4261 mL | 0.8522 mL | 2.1304 mL | |
| 30 mM | 0.0710 mL | 0.3551 mL | 0.7101 mL | 1.7754 mL | |
| 40 mM | 0.0533 mL | 0.2663 mL | 0.5326 mL | 1.3315 mL | |
| 50 mM | 0.0426 mL | 0.2130 mL | 0.4261 mL | 1.0652 mL | |
| 60 mM | 0.0355 mL | 0.1775 mL | 0.3551 mL | 0.8877 mL |
VLX1570 関連分類
HY-12471 関連分類
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