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341251

Sigma-Aldrich

Fascaplysin, Synthetic

A cell-permeable red pigment, originally isolated from marine sponge, that acts as a potent, ATP-competitive inhibitor of Cdk4/D1 (IC₅₀ = 0.35 µM).

Sinónimos:

Fascaplysin, Synthetic

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About This Item

Fórmula empírica (notación de Hill):
C18H11ClN2O
Número de CAS:
Peso molecular:
306.75
UNSPSC Code:
12352200

Quality Level

assay

≥98% (NMR)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
desiccated (hygroscopic)
protect from light

color

brown

solubility

methanol: 1 mg/mL
DMSO: 10 mg/mL

shipped in

ambient

storage temp.

2-8°C

InChI

1S/C18H10N2O.ClH/c21-18-13-6-2-4-8-15(13)20-10-9-12-11-5-1-3-7-14(11)19-16(12)17(18)20;/h1-10H;1H

InChI key

PWUOOJVYZQILBG-UHFFFAOYSA-N

General description

A cell-permeable red pigment, originally isolated from a species of marine sponge, that acts as a potent, ATP-competitive inhibitor of Cdk4/cyclin D1 (IC50 = 350 nM). Reported to inhibit Cdk6/cyclin D1 with much lower potency (IC50 = 3.4 µM). Exhibits little to no effect on the activities of several other Cdk′s (IC50 >20 µM) and tyrosine kinases (IC50 >10 µM). Biological effects are attributed, in part, to its ability to intercalate into DNA. Also displays anti-microbial activity.
A cell-permeable red pigment, originally isolated from marine sponge, that acts as a potent, ATP-competitive inhibitor of Cdk4/D1 (IC50 = 0.35 µM). It inhibits Cdk6/D1 with much lower potency (IC50 = 3.4 µM) and has been shown not to affect the activities of several other Cdk’s (IC50 >20 µM) and tyrosine kinases (IC50 >10 µM). Part of its biological effects may also be attributed to its ability to intercalate into DNA. Has also been shown to display anti-microbial activity.

Biochem/physiol Actions

Cell permeable: yes
Primary Target
CDK4/D1
Product competes with ATP.
Reversible: yes
Target IC50: 0.35 µM against Cdk4/D1

Packaging

Packaged under inert gas

Warning

Toxicity: Toxic (F)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Due to the nature of the Hazardous Materials in this shipment, additional shipping charges may be applied to your order. Certain sizes may be exempt from the additional hazardous materials shipping charges. Please contact your local sales office for more information regarding these charges.
Hormann, A., et al. 2001. Bioorg. Med. Chem.9, 917.
Kirsch, G., et al. 2000. J. Nat. Prod.63, 825.
Soni, R., et al. 2000. Biochem. Biophys. Res. Commun.275, 877.

Legal Information

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

Storage Class

11 - Combustible Solids

wgk_germany

WGK 1

flash_point_f

Not applicable

flash_point_c

Not applicable


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