Locostatin (Synonyms: UIC-1005)

Name: Locostatin
Brand: MedChemExpress
SKU: HY-W013411A
Rating: 4.5 (1 reviews)

Cat. No.: HY-W013411A Purity: 99.82%: FAQs
Data Sheet SDS COA Handling Instructions

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Locostatin (UIC-1005) is a potent RKIP inhibitor. Locostatin binds Raf kinase inhibitor RKIP protein and disrupts the interaction of RKIP with Raf-1 kinase and G protein-coupled receptor kinase 2. Locostatin inhibits cell proliferation and migration. Locostatin can be used to synthesize chemical probes toward PEBP-proteins. Locostatin aggravates thioacetamide (HY-Y0698)-induced acute liver failure in mice .

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

Locostatin Chemical Structure

CAS No. : 90719-30-5

Size	Price	Stock	Quantity
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 52	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 52	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 48	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 75	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 280	In-stock	Estimated Time of Arrival: December 31
100 mg		Get quote
200 mg		Get quote

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Based on 1 publication(s) in Google Scholar

Other Forms of Locostatin:

(E/Z)-Locostatin In-stock

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Description

IC₅₀ & Target

RKIP^[3]

In Vitro

Locostatin (200 µM; 37 °C; 6 h) disrupts the interaction of RKIP with Raf-1, and GRK2^[1].
Locostatin (50 µM; 0-48 h) inhibits cell proliferation and migration in MDCK cells^[2].

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

Cell Proliferation Assay^[2]

Cell Line:	MDCK cells
Concentration:	50 µM
Incubation Time:	0-48 h
Result:	Inhibited cell proliferation and sheet migration.

In Vivo

Locostatin (0.5 mg/kg; i.p.; once a day for 7 days) aggravates thioacetamide (HY-Y0698)-induced acute liver failure in mice^[3].

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

Animal Model:	6 weeks, 18-22 g, male ICR mice (TAA model; injected intraperitoneally with 300 mg/kg TAA once a day for 2 days)^[3]
Dosage:	0.5 mg/kg
Administration:	I.p.; once a day for 7 days
Result:	Decreased the expression of RKIP, led to more severe damage, such as steatosis and hepatic lesions, increased the production of ROS in the liver and TNF-α, IL-6 and IL-1β in the sera of mice with acute liver injury, inhibitd Nrf2 and HO-1 expression in the livers of mice, induced NF-κB activation in the livers of mice,increased the phosphorylation of JNK, p38 and ERK in liver tissues.

Molecular Weight

245.27

Formula

C₁₄H₁₅NO₃

CAS No.

90719-30-5

Appearance

Solid

Color

White to light yellow

SMILES

O=C1OC[C@H](CC2=CC=CC=C2)N1C(/C=C/C)=O

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 : 100 mg/mL (407.71 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	4.0771 mL	20.3857 mL	40.7714 mL
5 mM	0.8154 mL	4.0771 mL	8.1543 mL
10 mM	0.4077 mL	2.0386 mL	4.0771 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (10.19 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (10.19 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (10.19 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.82%

Select Batch:

Data Sheet (277 KB) SDS (251 KB)

COA (252 KB) HNMR (236 KB) LCMS (94 KB) OR (62 KB)

Handling Instructions (2659 KB)

References

[1]. Beshir AB, et al. Locostatin Disrupts Association of Raf Kinase Inhibitor Protein With Binding Proteins by Modifying a Conserved Histidine Residue in the Ligand-Binding Pocket. For Immunopathol Dis Therap. 2011;2(1):47-58. [Content Brief]

[2]. Mc Henry KT, et al. A non-antibacterial oxazolidinone derivative that inhibits epithelial cell sheet migration. Chembiochem. 2002 Nov 4;3(11):1105-11. [Content Brief]

[3]. Lin X, et al. Inhibition of RKIP aggravates thioacetamide-induced acute liver failure in mice. Exp Ther Med. 2018 Oct;16(4):2992-2998. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	4.0771 mL	20.3857 mL	40.7714 mL	101.9285 mL
	5 mM	0.8154 mL	4.0771 mL	8.1543 mL	20.3857 mL
	10 mM	0.4077 mL	2.0386 mL	4.0771 mL	10.1928 mL
	15 mM	0.2718 mL	1.3590 mL	2.7181 mL	6.7952 mL
	20 mM	0.2039 mL	1.0193 mL	2.0386 mL	5.0964 mL
	25 mM	0.1631 mL	0.8154 mL	1.6309 mL	4.0771 mL
	30 mM	0.1359 mL	0.6795 mL	1.3590 mL	3.3976 mL
	40 mM	0.1019 mL	0.5096 mL	1.0193 mL	2.5482 mL
	50 mM	0.0815 mL	0.4077 mL	0.8154 mL	2.0386 mL
	60 mM	0.0680 mL	0.3398 mL	0.6795 mL	1.6988 mL
	80 mM	0.0510 mL	0.2548 mL	0.5096 mL	1.2741 mL
	100 mM	0.0408 mL	0.2039 mL	0.4077 mL	1.0193 mL

Locostatin Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Locostatin90719-30-5UIC-1005UIC1005UIC 1005OthersRaf-1GRK2MDCK cellsTAA modelacute liver failureInhibitorinhibitorinhibit

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Locostatin (Synonyms: UIC-1005)

Customer Review

Other Forms of Locostatin:

Locostatin Related Antibodies

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

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Biological Activity

Purity & Documentation

References

Customer Review

Locostatin Related Antibodies

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Complete Stock Solution Preparation Table

Locostatin Related Classifications

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