2. Metabolic Enzyme/Protease Immunology/Inflammation
  3. Proteasome Interleukin Related
  4. PD 151746

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.

For research use only. We do not sell to patients.

PD 151746

PD 151746 Chemical Structure

CAS No. : 181765-30-0

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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Customer Review

Based on 7 publication(s) in Google Scholar

Other Forms of PD 151746:

PD 151746 Related Antibodies

Top Publications Citing Use of Products

View All Interleukin Related Isoform Specific Products:

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

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Description

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[1][2][3].

IC50 & Target[3]

IL-1α

 

In Vitro

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.

PD 151746 Related Antibodies

Cell Cytotoxicity Assay[2]

Cell Line: HMEC-1
Concentration: 2; 20 μM
Incubation Time: 24 h
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.

ELISA Assay[2]

Cell Line: HMEC-1
Concentration: 2; 20 μM
Incubation Time: 12 h
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.

Western Blot Analysis[2]

Cell Line: HMEC-1
Concentration: 20 μM
Incubation Time: 20 h
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.
In Vivo

PD 151746 (10 mg; i.p.; single injection) significantly reduces epidermal thickness and decreases mature IL-1α and calpain-1 protein levels to ameliorate Imiquimod (HY-B0180)-induced psoriatic skin lesions in mice[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/C (10-week-old) induced by Imiquimod[3]
Dosage: 10 mg
Administration: i.p.; single injection
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.
Molecular Weight

237.25

Formula

C11H8FNO2S
CAS No.
Appearance

Solid

Color

Light yellow to brown

SMILES

O=C(O)/C(S)=C/C1=CNC2=C1C=C(F)C=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.2150 mL 21.0748 mL 42.1496 mL
5 mM 0.8430 mL 4.2150 mL 8.4299 mL
View the 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.

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 95.03%

SDS (251 KB)

COA (251 KB) HNMR (272 KB) LCMS (297 KB)

Handling Instructions (2659 KB)
References

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
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PD 151746 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PD 151746181765-30-0PD151746PD-151746ProteasomeInterleukin RelatedILSH-SY5Y cellspapaincathepsin Btrypsincalmodulin-stimulated calcineurinHMEC-1 cellsthermolysinm-calpaincalpain-1μ-calpainInhibitorinhibitorinhibit

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