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BMS-3

Catalog No. T4600 CAS 1338247-30-5

BMS-3 is a potent LIMK inhibitor with IC50s of 5 nM and 6 nM for LIMK1 and LIMK2, respectively.

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BMS-3, CAS 1338247-30-5

Pack Size	Availability	Price/USD
1 mg	In stock	$ 35.00
2 mg	In stock	$ 48.00
5 mg	In stock	$ 75.00
10 mg	In stock	$ 119.00
25 mg	In stock	$ 243.00
50 mg	In stock	$ 405.00
100 mg	In stock	$ 590.00
1 mL * 10 mM (in DMSO)	In stock	$ 75.00

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Purity: 99.31%

Purity: 99.19%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	BMS-3 is a potent LIMK inhibitor with IC50s of 5 nM and 6 nM for LIMK1 and LIMK2, respectively.
Targets&IC50	LIMK1:5 nM, LIMK2:6 nM
In vitro	BMS-3 (Compound 2) exhibits a dose-dependent decrease in A549 human lung cancer cell viability by inducing mitotic arrest, characterized by enhanced total nuclear DNA intensity and histone H3 phosphorylation following a 24-hour exposure. It effectively inhibits these cells with an EC50 value of 154 nM[1]. Additionally, BMS-3 elucidates the role of LIMK1 in Cofilin phosphorylation; inhibition of p-LIMK by BMS-3 (1-50 μM) leads to a notable reduction in p-Cofilin levels after a 10-minute incubation under capacitating conditions, with a marked decrease in actin polymerization levels compared to the DMSO controls. Furthermore, under capacitating conditions, mouse sperm exposure to escalating concentrations of BMS-3 (0, 1, 10, and 50 μM) for 90 minutes significantly diminishes the percentage of sperm undergoing acrosomal exocytosis upon Progesterone stimulation[2], highlighting BMS-3's potential in affecting sperm functionality.
Kinase Assay	The protein kinase domains of human LIMK1 and LIMK2 are expressed as glutathione S-transferase fusion proteins using the Bac-to-Bac system in Sf9 cells. Compounds 1 to 6 (e.g., BMS-3) are assayed for inhibition of LIMK1 and LIMK2 protein kinase activity by radioactive phosphate incorporation into biotinylated full-length human destrin. Reactions are done with a concentration series of compound in 25 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 5 mM MnCl2, 1 μM total ATP, 83 μg/mL biotinylated destrin, 167 ng/mL glutathione S-transferase-LIMK1, or 835 ng/mL glutathione S-transferase-LIMK2 in a total volume of 60 μL at room temperature for 30 min (LIMK1) or 60 min (LIMK2). Reactions are terminated by addition of 140 μL of 20% TCA/100 mM sodium pyrophosphate, and the precipitates are harvested onto GF/C unifilter plates. The radioactivity incorporated is determined using a TopCount after addition of 35 μL Microscint scintillation fluid[1]

Molecular Weight	429.27
Formula	C17H12Cl2F2N4OS
CAS No.	1338247-30-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 27.5 mg/mL (64.06 mM)

References and Literature

1. Ross-Macdonald P, et al. Identification of a nonkinase target mediating cytotoxicity of novel kinase inhibitors. Mol Cancer Ther. 2008 Nov;7(11):3490-8. 2. Romarowski A, et al. PKA-dependent phosphorylation of LIMK1 and Cofilin is essential for mouse sperm acrosomal exocytosis. Dev Biol. 2015 Sep 15;405(2):237-49.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Kinase Inhibitor Library Anti-Aging Compound Library Bioactive Compound Library Bioactive Compounds Library Max Cell Cycle Compound Library NO PAINS Compound Library Anti-Cancer Compound Library Target-Focused Phenotypic Screening Library

Related Products

Related compounds with same targets

LY2812223 LX7101 BMS-5 SM1-71 R-10015 T56-LIMKi TH-257 LIMK-IN-22j

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Keywords

BMS-3 1338247-30-5 Cell Cycle/Checkpoint LIM Kinase BMS 3 inhibit Inhibitor LIMKs BMS3 LIM Kinase (LIMK) inhibitor

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