1. Autophagy
  2. ULK

MRT68921 hydrochloride 

Cat. No.: HY-100006A Purity: 99.71%
Handling Instructions

MRT68921 hydrochloride 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 hydrochloride Chemical Structure

MRT68921 hydrochloride Chemical Structure

CAS No. : 2080306-21-2

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in Water USD 79 In-stock
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Estimated Time of Arrival: December 31
5 mg USD 72 In-stock
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10 mg USD 120 In-stock
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Estimated Time of Arrival: December 31
25 mg USD 240 In-stock
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50 mg USD 432 In-stock
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Estimated Time of Arrival: December 31
100 mg USD 564 In-stock
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Estimated Time of Arrival: December 31
200 mg USD 1020 In-stock
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500 mg   Get quote  
1 g   Get quote  

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Other Forms of MRT68921 hydrochloride:

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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

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].

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 2.1230 mL 10.6148 mL 21.2296 mL
5 mM 0.4246 mL 2.1230 mL 4.2459 mL
10 mM 0.2123 mL 1.0615 mL 2.1230 mL
Please refer to the solubility information to select the appropriate solvent.
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

471.04

Formula

C₂₅H₃₅ClN₆O

CAS No.

2080306-21-2

SMILES

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

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

H2O: 10 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.71%

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