1. Cell Cycle/DNA Damage
  2. LIM Kinase (LIMK)
  3. R-10015

R-10015 

Cat. No.: HY-120097 Purity: 99.07%
Handling Instructions

R-10015, a broad-spectrum antiviral compound for HIV infection, acts as a potent and selective inhibitor of LIM domain kinase (LIMK) and binds to the ATP-binding pocket, with an IC50 of 38 nM for human LIMK1.

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

R-10015 Chemical Structure

R-10015 Chemical Structure

CAS No. : 2097938-51-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 385 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 550 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1650 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2200 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Description

R-10015, a broad-spectrum antiviral compound for HIV infection, acts as a potent and selective inhibitor of LIM domain kinase (LIMK) and binds to the ATP-binding pocket, with an IC50 of 38 nM for human LIMK1[1].

IC50 & Target[1]

human LIMK1

38 nM (IC50)

In Vitro

R-10015 (100 μM; 0-4 hours) inhibits cofilin phosphorylation directly through blocking LIM kinase in CEM-SS T cells[1].
R-10015 inhibits HIV-1 DNA synthesis, nuclear migration, and virion release[1].
R-10015 inhibits multiple viruses, including Zaire ebolavirus (EBOV), Rift Valley fever virus (RVFV), Venezuelan equine encephalitis virus (VEEV), and herpes simplex virus 1 (HSV-1) [1].

Western Blot Analysis[1]

Cell Line: CEM-SS T cells
Concentration: 100 μM
Incubation Time: 0 hour,0.5 hour,1 hour,2 hours,4 hours
Result: Inhibited cofilin phosphorylation directly through blocking LIM kinase in CEM-SS T cells.
In Vivo

R-10015 (10 mg/kg; i.p.) displays none indication of toxicity. The result suggests the possibility of short-term use of LIMK inhibitors to block viral infections[1].

Animal Model: 6-8 weeks female C3H/HeN mice[1]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection
Result: Displayed none indication of toxicity.
Molecular Weight

410.86

Formula

C₂₀H₁₉ClN₆O₂

CAS No.

2097938-51-5

SMILES

O=C(C1=CC=C2NC(C3CCN(C4=C5C(NC=C5Cl)=NC=N4)CC3)=NC2=C1)OC

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (152.12 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4339 mL 12.1696 mL 24.3392 mL
5 mM 0.4868 mL 2.4339 mL 4.8678 mL
10 mM 0.2434 mL 1.2170 mL 2.4339 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.06 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.08 mg/mL (5.06 mM); Suspended solution; Need ultrasonic

*All of the co-solvents are provided by MCE.
References

Purity: 99.07%

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R-10015
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