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BMS-5

Catalog No. T4598 CAS 1338247-35-0

Synonyms: BMS5, LIMKi 3

BMS-5 (LIMKi 3) is a potent LIMK inhibitor with IC50s of 7 nM and 8 nM for LIMK1 and LIMK2, respectively.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

BMS-5, CAS 1338247-35-0

Pack Size	Availability	Price/USD
1 mg	In stock	$ 36.00
2 mg	In stock	$ 50.00
5 mg	In stock	$ 76.00
10 mg	In stock	$ 125.00
25 mg	In stock	$ 209.00
50 mg	In stock	$ 313.00
100 mg	In stock	$ 467.00
1 mL * 10 mM (in DMSO)	In stock	$ 84.00

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Purity: 99.88%

Purity: 95.83%

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Storage & Solubility Information

Description	BMS-5 (LIMKi 3) is a potent LIMK inhibitor with IC50s of 7 nM and 8 nM for LIMK1 and LIMK2, respectively.
Targets&IC50	LIMK1:7 nM, LIMK2:8 nM
In vitro	BMS-5 inhibits cofilin-Ser3 phosphorylation in a dose-dependent manner in Nf2ΔEx2 mouse Schwann cells (MSCs) with an IC50 of ~2 μM. BMS-5 reduces Nf2ΔEx2 MSC viability in a dose-dependent manner with an IC50 of 3.9 μM, but does not significantly reduce the viability of control Nf2flox2/flox2 MSCs at equivalent BMS-5 concentrations. At 10 μM BMS-5, Nf2ΔEx2 MSC viability is 40% compared to 83% for controls[2] .
In vivo	BMS-5 (20 or 200 μM/side) was administered bilaterally into the hippocampi of rats immediately following contextual fear conditioning training. Memory consolidation was assessed 48 hours after the conditioning through tests measuring freezing behavior. Analysis revealed that rats receiving the 200 μM dose of BMS-5 exhibited significantly reduced freezing compared to those treated with 20 μM and the control group [P].
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-5) 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]
Cell Research	Cell membrane asymmetry is measured. Nf2ΔEx2 MSCs plated in a 6-well format are incubated with 2 μM BMS-5 or DMSO vehicle for 24 hrs. Cell are harvested and assayed. Plasma membrane asymmetry is evaluated with the Violet ratiometric assay by flow cytometry[2] .
Animal Research	Rats [3]

Synonyms	BMS5, LIMKi 3
Molecular Weight	431.29
Formula	C17H14Cl2F2N4OS
CAS No.	1338247-35-0

Storage

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

Solubility Information

DMSO: 55 mg/mL (127.52 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. Petrilli A, et al. LIM Domain Kinases as Potential Therapeutic Targets for Neurofibromatosis Type 2.Oncogene. Oncogene. 2014 Jul 3;33(27):3571-82. 3. Lunardi P, et al. Effects of Hippocampal LIMK Inhibition on Memory Acquisition, Consolidation, Retrieval, Reconsolidation, and Extinction. Mol Neurobiol. 2017 Jan 13. 4. Gao T T, Wang Y, Liu L, et al. LIMK1/2 in the mPFC plays a role in chronic stress-induced depressive-like effects in mice[J]. International Journal of Neuropsychopharmacology. 2020, 23(12): 821-836.

Citations

1. Gao T T, Wang Y, Liu L, et al. LIMK1/2 in the mPFC plays a role in chronic stress-induced depressive-like effects in mice. International Journal of Neuropsychopharmacology. 2020, 23(12): 821-836.

Related compound libraries

This product is contained In the following compound libraries：

Kinase Inhibitor Library Anti-Cancer Compound Library NO PAINS Compound Library Target-Focused Phenotypic Screening Library

Related Products

Related compounds with same targets

LY2812223 LX7101 SM1-71 BMS-3 T56-LIMKi R-10015 TH-257 LIMK-IN-22j

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Keywords

BMS-5 1338247-35-0 Cell Cycle/Checkpoint LIM Kinase LIMKi3 BMS5 inhibit LIM Kinase (LIMK) LIMKs Inhibitor BMS 5 LIMKi 3 LIMKi-3 inhibitor

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