1. Autophagy
  2. ULK

MRT68921 

Cat. No.: HY-100006
Handling Instructions

MRT68921 is the most 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 Chemical Structure

MRT68921 Chemical Structure

CAS No. : 1190379-70-4

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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

IC50 & Target

IC50: 2.9 nM (ULK1), 1.1 nM(ULK2)[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].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3011 mL 11.5054 mL 23.0107 mL
5 mM 0.4602 mL 2.3011 mL 4.6021 mL
10 mM 0.2301 mL 1.1505 mL 2.3011 mL
*Please refer to the solubility information to select the appropriate solvent.
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, supplemented with 10% fetal bovine serum and penicillin/streptomycin, and cultured at 37°C, 5% CO2. 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
Molecular Weight

434.58

Formula

C₂₅H₃₄N₆O

CAS No.

1190379-70-4

SMILES

O=C(C1CCC1)NCCCNC2=NC(NC3=CC4=C(CN(C)CC4)C=C3)=NC=C2C5CC5

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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MRT68921
Cat. No.:
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MRT68921

Cat. No.: HY-100006