MRT68921 dihydrochloride

Name: MRT68921 dihydrochloride
Brand: MedChemExpress
SKU: HY-100006A
Rating: 5.0 (17 reviews)

Cat. No.: HY-100006A Purity: 99.67%: FAQs
Data Sheet SDS COA Handling Instructions

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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

CAS No. : 2080306-21-2

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water ready for reconstitution	USD 80	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in Water	USD 80	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 34	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 72	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 120	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 240	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 432	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 564	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 17 publication(s) in Google Scholar

Other Forms of MRT68921 dihydrochloride:

MRT68921 Get quote
MRT68921 hydrochloride Get quote

17 Publications Citing Use of MCE MRT68921 dihydrochloride

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ULK1 ULK2

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.

2080306-21-2

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
10 mM	0.1970 mL	0.9852 mL	1.9704 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.

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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

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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μL

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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: 99.67%

Select Batch:

Data Sheet (273 KB) SDS (393 KB)

COA (246 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[1]. Petherick KJ, et al. Pharmacological inhibition of ULK1 kinase blocks mammalian target of rapamycin (mTOR)-dependent autophagy. J Biol Chem. 2015 May 1;290(18):11376-83. [Content Brief]

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	[1]. Petherick KJ, et al. Pharmacological inhibition of ULK1 kinase blocks mammalian target of rapamycin (mTOR)-dependent autophagy. J Biol Chem. 2015 May 1;290(18):11376-83. [Content Brief]

Complete Stock Solution Preparation Table

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.