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  3. MRT68921 dihydrochloride

MRT68921 dihydrochloride is a potent inhibitor of ULK1 and ULK2, with IC50 values of 2.9 nM and 1.1 nM, respectively.

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

MRT68921 dihydrochloride Chemical Structure

MRT68921 dihydrochloride Chemical Structure

CAS No. : 2080306-21-2

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in Water
ready for reconstitution
USD 80 In-stock
Solution
10 mM * 1 mL in Water USD 80 In-stock
Solid
1 mg USD 34 In-stock
5 mg USD 72 In-stock
10 mg USD 120 In-stock
25 mg USD 240 In-stock
50 mg USD 432 In-stock
100 mg USD 564 In-stock
200 mg USD 1020 In-stock
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Customer Review

Based on 13 publication(s) in Google Scholar

Other Forms of MRT68921 dihydrochloride:

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

MRT68921 dihydrochloride is a potent inhibitor of ULK1 and ULK2, with IC50 values of 2.9 nM and 1.1 nM, respectively[1].

In Vitro

ULK1, a serine/threonine protein kinase, is essential for the initial stages of autophagy. MRT68921 inhibits ULK1 and ULK2 in vitro and block autophagy in cells. MRT68921 is the most potent inhibitor of both ULK1 and ULK2, with greater than a 15-fold reduction in the IC50 for ULK1 (2.9 nm) and greater than a 30-fold reduction for ULK2 (1.1 nm). Autophagy-inhibiting capacity of the compounds is specifically through ULK1. ULK1 inhibition results in accumulation of stalled early autophagosomal structures, indicating a role for ULK1 in the maturation of autophagosomes as well as initiation[1].

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

Molecular Weight

507.50

Formula

C25H36Cl2N6O

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

[H]Cl.O=C(C1CCC1)NCCCNC2=NC(NC3=CC4=C(CN(C)CC4)C=C3)=NC=C2C5CC5.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : 20.83 mg/mL (41.04 mM; ultrasonic and warming and heat to 60°C)

DMSO : 8.33 mg/mL (16.41 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 1.9704 mL 9.8522 mL 19.7044 mL
5 mM 0.3941 mL 1.9704 mL 3.9409 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, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

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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
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Purity & Documentation

Purity: 99.58%

References
Kinase Assay
[1]

Kinase assays are carried out in 50 mM Tris-HCl, pH 7.4, 10 mM magnesium acetate, 0.1 mM EGTA, and 0.1% β-mercaptoethanol, containing 30 μM cold ATP, and 0.5 μCi of [γ-32P]ATP for 5 min at 25 °C. Prior to ATP addition, reaction mixes are pre-warmed to 25 °C for 5 min. Reactions are stopped by the addition of sample buffer, followed by SDS-PAGE, transfer to nitrocellulose, and analysis by autoradiography and immunoblot[1].

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

Cell Assay
[1]

MEFs and 293T cells are grown in DMEM. For induction of autophagy, cells are typically grown to 75% confluency, ished twice, and incubated in Earle's balanced salt solution (EBSS) for 1 h (or complete medium as a control). MRT67307 (10 μM), MRT68921 (1 μM), AZD8055 (1 μM), or bafilomycin A1 (50 nM) is included[1].

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

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, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 1.9704 mL 9.8522 mL 19.7044 mL 49.2611 mL
5 mM 0.3941 mL 1.9704 mL 3.9409 mL 9.8522 mL
10 mM 0.1970 mL 0.9852 mL 1.9704 mL 4.9261 mL
15 mM 0.1314 mL 0.6568 mL 1.3136 mL 3.2841 mL
H2O 20 mM 0.0985 mL 0.4926 mL 0.9852 mL 2.4631 mL
25 mM 0.0788 mL 0.3941 mL 0.7882 mL 1.9704 mL
30 mM 0.0657 mL 0.3284 mL 0.6568 mL 1.6420 mL
40 mM 0.0493 mL 0.2463 mL 0.4926 mL 1.2315 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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MRT68921 dihydrochloride Related Classifications

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  • 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.

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Product Name:
MRT68921 dihydrochloride
Cat. No.:
HY-100006A
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