2. Metabolic Enzyme/Protease
  3. Glutathione S-transferase
  4. LAS17

LAS17 is a potent and selective tyrosine-directed irreversible inhibitor for glutathione?S-Transferase Pi (GSTP1) . LAS17 inhibits GSTP1 activity with an IC50 of 0.5 μM. LAS17 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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

LAS17 Chemical Structure

LAS17 Chemical Structure

CAS No. : 2362527-67-9

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Oil + Solvent
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 308 In-stock
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5 mg USD 280 In-stock
10 mg USD 450 In-stock
25 mg USD 940 In-stock
50 mg USD 1500 In-stock
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Based on 1 publication(s) in Google Scholar

LAS17 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE LAS17

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

LAS17 is a potent and selective tyrosine-directed irreversible inhibitor for glutathione?S-Transferase Pi (GSTP1) [1]. LAS17 inhibits GSTP1 activity with an IC50 of 0.5 μM[2]. LAS17 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

In Vitro

Glutathione S-Transferase Pi (GSTP1) mediates cellular defense against reactive electrophiles. LAS17 inhibits GSTP1 activity in vitro in a concentration-dependent manner[1]. 
LAS17 (10 µM; Serum-free survival 48 h) treatment in 231MFP breast cancer cells recapitulates the serum-free cell survival impairments observed with genetic inactivation of GSTP1[2]. 
GSTP1 knockdown in LAS17 (10 µM) treatment in 231MFP cells results in increased levels of phosphorylated AMPK and acetyl CoA carboxylase (ACC)[2].
LAS17 treatment in 231MFP cells also shows reduced levels of ATP, lactic acid, purine nucleotides, and diacylated phospholipids and alkylacyl ether lipids and increased levels of acyl carnitines (ACs), ceramides, lysophospholipids[2].

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

LAS17 Related Antibodies

Cell Viability Assay[2]

Cell Line: 231MFP breast cancer cells
Concentration: 10 µM
Incubation Time: 48 hours
Result: Recapitulated the serum-free cell survival impairments observed with genetic inactivation of GSTP1.

Western Blot Analysis[2]

Cell Line: 231MFP cells
Concentration: 10 µM
Incubation Time:
Result: LAS17-treated 231MFP cells show increased levels of phosphorylated AMPK and ACC.
In Vivo

Daily administration of LAS17 (20 mg/kg ip, once per day) significantly impairs 231MFP breast tumor xenograft growth in immune-deficient mice when treatment is initiated 2 days after subcutaneous injection of cells, and LAS17 even slows tumor growth when initiated 16 days after tumor implantation, with no observable toxicity and no weight-change[2].

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

Animal Model: Severe combined immunodeficiency (SCID) mice bearing 231MFP tumor xenograft[2]
Dosage: 20 mg/kg (prepared in PBS:ethanol:PEG40 (18:1:1))
Administration: Daily administration i.p., once per day
Result: Significantly impaired 231MFP breast tumor xenograft growth.
Molecular Weight

359.25

Formula

C15H20Cl2N4O2
CAS No.
Appearance

Oil

Color

Colorless to light yellow

SMILES

CC(C)C[C@H](C(OC)=O)N(C1=NC(Cl)=NC(Cl)=N1)CCCC#C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Pure form -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (278.36 mM; Need ultrasonic; 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 2.7836 mL 13.9179 mL 27.8358 mL
5 mM 0.5567 mL 2.7836 mL 5.5672 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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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7836 mL 13.9179 mL 27.8358 mL 69.5894 mL
5 mM 0.5567 mL 2.7836 mL 5.5672 mL 13.9179 mL
10 mM 0.2784 mL 1.3918 mL 2.7836 mL 6.9589 mL
15 mM 0.1856 mL 0.9279 mL 1.8557 mL 4.6393 mL
20 mM 0.1392 mL 0.6959 mL 1.3918 mL 3.4795 mL
25 mM 0.1113 mL 0.5567 mL 1.1134 mL 2.7836 mL
30 mM 0.0928 mL 0.4639 mL 0.9279 mL 2.3196 mL
40 mM 0.0696 mL 0.3479 mL 0.6959 mL 1.7397 mL
50 mM 0.0557 mL 0.2784 mL 0.5567 mL 1.3918 mL
60 mM 0.0464 mL 0.2320 mL 0.4639 mL 1.1598 mL
80 mM 0.0348 mL 0.1740 mL 0.3479 mL 0.8699 mL
100 mM 0.0278 mL 0.1392 mL 0.2784 mL 0.6959 mL
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LAS17 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:

LAS172362527-67-9LAS 17LAS-17Glutathione S-transferaseGlutathione transferasesGSTsirreversibleglutathione,?S-TransferaseGSTP1231MFPbreastcancerInhibitorinhibitorinhibit

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