PD 151746
Based on 7 publication(s) in Google Scholar
PD 151746 is a selective calpain-1 inhibitor with an IC50 of 260 nM. PD 151746 binds μ-calpain Ca2+-binding sites, and shows selectivity over cathepsin B, papain, trypsin, thermolysin, and basal calcineurin. PD 151746 reduces Oxidized low-density lipoprotein (oxLDL)-induced cytotoxicity, apoptotic DNA fragmentation, and blocks IL-1α maturation. PD 151746 can be used for the research of atherosclerosis and psoriasis.
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- 純度: 95.0%
- CAS 番号: 181765-30-0
- 分子式: C11H8FNO2S
- 分子量:237.25
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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
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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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MedChemExpress（MCE）の使用を引用している文献 PD 151746
More- ACS Sens. 2026 Mar 27;11(3):1891-1907. [Abstract]
- Basic Res Cardiol. 2022 Aug 23;117(1):40. [Abstract]
- Microbiol Res. 2024 Dec:289:127916. [Abstract]
- CNS Neurosci Ther. 2024 Feb;30(2):e14365. [Abstract]
- J Cell Mol Med. 2020 Aug;24(16):9287-9299. [Abstract]
- Thorac Cancer. 2022 Jun;13(12):1772-1782. [Abstract]
- Research Square Preprint. 2020 Sep.
生物活性
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IL-1α |
PD 151746 potently and selectively inhibits μ-calpain with an apparent Ki of 0.26 μM, shows 20-fold selectivity over m-calpain[1].
PD 151746 (10 μM; 2 h) effectively inhibits calpain activity in Maitotoxin-treated human neuroblastoma SH-SY5Y cells[1].
PD 151746 (2-20 μM; 24 h) dose-dependently reduces oxLDL-induced cytotoxicity in HMEC-1 cells[2].
PD 151746 (2-20 μM; 12 h) significantly reduces oxLDL-induced apoptotic nucleosomal DNA fragmentation in HMEC-1 cells at 20 μM[2].
PD 151746 (20 μM; 20 h) inhibits oxLDL-induced calpain-mediated cleavage of α-fodrin in HMEC-1 cells[2].
PD 151746 (20 μM; 20 h) inhibits oxLDL-induced calpain-mediated cleavage of Bid in HMEC-1 cells[2].
PD 151746 (15 μM) blocks hS100A7-induced mature IL-1α production in normal human epidermal keratinocytes, and it inhibits calpain-1 with an IC50 of 260 nM and 20-fold selectivity over calpain-2[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HMEC-1
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Concentration:2; 20 μM
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Incubation Time:24 h
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Result:Reduced oxLDL-induced cytotoxicity by approximately 40% at 20 μM compared to oxLDL-only treatment, with a statistically significant effect.
Reduced cytotoxicity to a lesser extent at 2 μM compared to the 20 μM concentration.
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Cell Line:HMEC-1
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Concentration:2; 20 μM
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Incubation Time:12 h
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Result:Caused a statistically significant reduction in oxLDL-induced nucleosomal DNA fragmentation at 20 μM.
Exerted a smaller, non-significant effect on oxLDL-induced nucleosomal DNA fragmentation at 2 μM.
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Cell Line:HMEC-1
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Concentration:20 μM
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Incubation Time:20 h
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Result:Prevented oxLDL-induced formation of the calpain-specific 150 kDa α-fodrin fragment.
Reduced the ratio of calpain-generated to caspase-generated α-fodrin fragments (A150/A120) from 1.99 in oxLDL-only treated cells to a level consistent with untreated cells.\n
Prevented oxLDL-induced reduction of full-length 22 kDa Bid.
Maintained the ratio of Bid to α-tubulin at a level comparable to untreated control cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/C (10-week-old) induced by Imiquimod[3]
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Dosage:10 mg
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Administration:i.p.; single injection
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Result:Ameliorated psoriatic lesions and reversed epidermal hyperplasia.
Significantly reduced epidermal thickness compared to imiquimod-only controls.
Decreased mature IL-1α and calpain-1 protein expression in psoriasis-like lesions.
Left IL-1α mRNA expression unchanged.
化学情報
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CAS 番号 181765-30-0
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性状 Solid
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分子量 237.25
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分子式 C11H8FNO2S
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Color Light yellow to brown
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SMILES
O=C(O)/C(S)=C/C1=CNC2=C1C=C(F)C=C2
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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 (7)
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Journal Impact Factor
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Most Recent
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ACS Sens
A Sensitive Green-Red FRET Sensor for Calpain-1 Utilizing Heterodimeric Fluorescent Proteins from Distinct Evolutionary Origins. [Abstract]2026 Mar 27;11(3):1891-1907. PMID: 41837894 -
Basic Res Cardiol
Mitochondrial calpain-1 activates NLRP3 inflammasome by cleaving ATP5A1 and inducing mitochondrial ROS in CVB3-induced myocarditis. [Abstract]2022 Aug 23;117(1):40. PMID: 35997820 -
Microbiol Res
Inhibition of calpain reduces oxidative stress and attenuates pyroptosis and ferroptosis in Clostridium perfringens Beta-1 toxin-induced macrophages. [Abstract]2024 Dec:289:127916. PMID: 39342748 -
CNS Neurosci Ther
Enriched environment ameliorates fear memory impairments induced by sleep deprivation via inhibiting PIEZO1/calpain/autophagy signaling pathway in the basal forebrain. [Abstract]2024 Feb;30(2):e14365. PMID: 37485782 -
J Cell Mol Med
Calpain-2 plays a pivotal role in the inhibitory effects of propofol against TNF-α-induced autophagy in mouse hippocampal neurons. [Abstract]2020 Aug;24(16):9287-9299. PMID: 32627970 -
Thorac Cancer
ACT001 inhibits the proliferation of non-small cell lung cancer cells by upregulating NKTR expression. [Abstract]2022 Jun;13(12):1772-1782. PMID: 35537816 -
溶剤 & 溶解度
DMSO : 50 mg/mL (210.75 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (282 KB)
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SDS (251 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Wang KK, et al. An alpha-mercaptoacrylic acid derivative is a selective nonpeptide cell-permeable calpain inhibitor and is neuroprotective. Proc Natl Acad Sci U S A. 1996;93(13):6687-6692. [Content Brief]
[2]. Pörn-Ares MI, et al. Oxidized low-density lipoprotein induces calpain-dependent cell death and ubiquitination of caspase 3 in HMEC-1 endothelial cells. Biochem J. 2003 Sep 1;374(Pt 2):403-11. [Content Brief]
[3]. Lei H, et al. Human S100A7 Induces Mature Interleukin1α Expression by RAGE-p38 MAPK-Calpain1 Pathway in Psoriasis. PLoS One. 2017;12(1):e0169788. Published 2017 Jan 6. [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 | 4.2150 mL | 21.0748 mL | 42.1496 mL | 105.3741 mL |
| 5 mM | 0.8430 mL | 4.2150 mL | 8.4299 mL | 21.0748 mL | |
| 10 mM | 0.4215 mL | 2.1075 mL | 4.2150 mL | 10.5374 mL | |
| 15 mM | 0.2810 mL | 1.4050 mL | 2.8100 mL | 7.0249 mL | |
| 20 mM | 0.2107 mL | 1.0537 mL | 2.1075 mL | 5.2687 mL | |
| 25 mM | 0.1686 mL | 0.8430 mL | 1.6860 mL | 4.2150 mL | |
| 30 mM | 0.1405 mL | 0.7025 mL | 1.4050 mL | 3.5125 mL | |
| 40 mM | 0.1054 mL | 0.5269 mL | 1.0537 mL | 2.6344 mL | |
| 50 mM | 0.0843 mL | 0.4215 mL | 0.8430 mL | 2.1075 mL | |
| 60 mM | 0.0702 mL | 0.3512 mL | 0.7025 mL | 1.7562 mL | |
| 80 mM | 0.0527 mL | 0.2634 mL | 0.5269 mL | 1.3172 mL | |
| 100 mM | 0.0421 mL | 0.2107 mL | 0.4215 mL | 1.0537 mL |
PD 151746 関連分類
HY-19749 関連分類
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