341251

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).

• Synonym(s): Fascaplysin, Synthetic
• Empirical Formula (Hill Notation): C₁₈H₁₁ClN₂O
• CAS Number: 114719-57-2
• Molecular Weight: 306.75
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• 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

Description

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

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 1
• flash_point_f: Not applicable
• flash_point_c: Not applicable