1. Cell Cycle/DNA Damage
  2. LIM Kinase (LIMK)

BMS-5 (Synonyms: LIMKI 3)

Cat. No.: HY-18305 Purity: 99.89%
Handling Instructions

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

For research use only. We do not sell to patients.

BMS-5 Chemical Structure

BMS-5 Chemical Structure

CAS No. : 1338247-35-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 132 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
10 mg USD 180 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
50 mg USD 528 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
100 mg USD 948 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Related Small Molecules:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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

IC50 & Target[1]

LIMK1

7 nM (IC50)

LIMK2

8 nM (IC50)

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) is bilaterally infused into the hippocampus of rats immediately after contextual fear conditioning training. Rats are tested for memory consolidation 48 h after fear conditioning. Post hoc analysis shows that the group treated with 200 μM BMS-5 express lower freezing levels compared to the 20 μM and vehicle groups (P<0.01)[3].

Solvent & Solubility
In Vitro: 

DMSO : ≥ 34 mg/mL (78.83 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3186 mL 11.5931 mL 23.1863 mL
5 mM 0.4637 mL 2.3186 mL 4.6373 mL
10 mM 0.2319 mL 1.1593 mL 2.3186 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[2]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[3]

Rats [3]
Male Wistar rats (age 2-3 months, weight 290-350 g) are used. BMS-5 is prepared in a vehicle solution (1% DMSO in sterile isotonic saline). At the time of infusion, a 30-gauge infusion needle is fitted into a guide cannula, with its tip protruding 1.0 mm beyond the guide cannula end and aimed at the pyramidal cell layer of CA1 of the dorsal hippocampus. Avolume of 1 μL of BMS-5 (20 and 200 μM) or vehicle (DMSO 1%) is bilaterally infused in a time of 90 s. The doses of BMS-5 are based on its IC50 value and in vitro studies.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

431.29

Formula

C₁₇H₁₄Cl₂F₂N₄OS

CAS No.

1338247-35-0

SMILES

CC(C)C(NC1=NC=C(C2=CC(C(F)F)=NN2C3=C(Cl)C=CC=C3Cl)S1)=O

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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BMS-5
Cat. No.:
HY-18305
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BMS-5

Cat. No.: HY-18305