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Merck

513022

PD 150606

A cell-permeable, non-competitive, selective non-peptide calpain inhibitor [Ki = 210 nM for calpain-1 and 370 nM for calpain-2.

Synonym(s):

PD 150606, 3-(4-Iodophenyl)-2-mercapto-(Z)-2-propenoic Acid

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About This Item

Empirical Formula (Hill Notation):
C9H7IO2S
CAS Number:
426821-41-2
Molecular Weight:
306.12
MDL number:
MFCD00011966
NACRES:
NA.77
UNSPSC Code:
12352200

Product Name

PD 150606, A cell-permeable, non-competitive, selective non-peptide calpain inhibitor [Ki = 210 nM for calpain-1 and 370 nM for calpain-2.

assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

off-white

solubility

DMSO: 100 mg/mL
methanol: 25 mg/mL

shipped in

ambient

storage temp.

−20°C

Quality Level

100

Related Categories

Biochem/physiol Actions

Cell permeable: yes
Primary Target
Calpain-1
Product does not compete with ATP.
Reversible: no
Target Ki: 210 nM for calpain-1 and 370 nM for calpain-2

Disclaimer

Toxicity: Standard Handling (A)

General description

A cell-permeable, non-competitive, selective non-peptide calpain inhibitor [Ki = 210 nM for calpain-1 (Cat. Nos. 208712 and 208713) and 370 nM for calpain-2 (Cat. Nos. 208715 and 208718)] directed towards the calcium binding sites of calpain. Exhibits high specificity for calpains relative to other proteases, such as cathepsin B and cathepsin L. Does not shield calpain against inactivation by the active-site inhibitor trans-(epoxysuccinyl)-L-leucyl-amido-3-methylbutane. Reportedly prevents dexamethasone-induced apoptosis in thymocytes.
A cell-permeable, selective non-peptide calpain inhibitor (Ki = 210 nM for calpain I and 370 nM for calpain II) directed towards the calcium- binding sites of calpain. Exhibits high specificity for calpains relative to other proteases, such as cathepsin B and L. PD 150606 is a non-competitive inhibitor with respect to the substrate and does not shield calpain against inactivation by the active-site inhibitor trans-(epoxysuccinyl)-L-leucyl-amido-3-methylbutane. Reportedly prevents dexamethasone-induced apoptosis of thymocytes.

Other Notes

Lin, G.D., et al. 1997. Nat. Struct. Biol. 4, 539.
Squier, M.K., and Cohen, J.J. 1997. J. Immunol. 158, 3960.
Edelstein, C.L., et al. 1996. Kidney Int. 50, 1150.
Wang, K.K.W., et al. 1996. Proc. Natl. Acad. Sci. USA 93, 6687.

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class

11 - Combustible Solids

wgk

WGK 1

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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Mehmet Şerif Aydın et al.
iScience, 26(10), 107715-107715 (2023-09-13)
Trauma, vascular events, or neurodegenerative processes can lead to axonal injury and eventual transection (axotomy). Neurons can survive axotomy, yet the underlying mechanisms are not fully understood. Excessive water entry into injured neurons poses a particular risk due to swelling

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