2. Autophagy
  3. ULK Autophagy
  4. MR-2088

MR-2088 is a reversible, ATP-competitive, and selective ULK1/2 inhibitor with pEC50 values of 8.3 and 8.7 respectively. MR-2088 effectively inhibits autophagic flux and demonstrates a synergistic antiproliferative effect with Trametinib (HY-10999) (MEK inhibitor) in vitro. MR-2088 can be used for non-small lung cell cancer (NSCLC) research.

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

MR-2088

MR-2088 Chemical Structure

CAS No. : 2922531-69-7

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

MR-2088 Related Antibodies

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Description

MR-2088 is a reversible, ATP-competitive, and selective ULK1/2 inhibitor with pEC50 values of 8.3 and 8.7 respectively. MR-2088 effectively inhibits autophagic flux and demonstrates a synergistic antiproliferative effect with Trametinib (HY-10999) (MEK inhibitor) in vitro. MR-2088 can be used for non-small lung cell cancer (NSCLC) research[1].

IC50 & Target[1]

ULK1

8.3 (pEC50)

ULK2

8.7 (pEC50)

Cellular Effect
Cell Line Type Value Description References
NCI-H2030 EC50
36 nM
Compound: 43; MR-2088
Inhibition of autophagy in human NCI-H2030 cells assessed as inhibition of ATG13 phosphorylation at Ser318 residue incubated for 24 hrs in aminoacid starving medium by Western blot analysis
Inhibition of autophagy in human NCI-H2030 cells assessed as inhibition of ATG13 phosphorylation at Ser318 residue incubated for 24 hrs in aminoacid starving medium by Western blot analysis
[PMID: 38232465]
NCI-H2030 EC50
48 nM
Compound: 43; MR-2088
Inhibition of autophagy in trametinib treated human NCI-H2030 cells assessed as inhibition of ATG13 phosphorylation at Ser318 residue incubated for 24 hrs by Western blot analysis
Inhibition of autophagy in trametinib treated human NCI-H2030 cells assessed as inhibition of ATG13 phosphorylation at Ser318 residue incubated for 24 hrs by Western blot analysis
[PMID: 38232465]
NCI-H2030 IC50
3.2 μM
Compound: 43; MR-2088
Antiproliferative activity against human NCI-H2030 cells harboring KRAS G12C mutant assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay
Antiproliferative activity against human NCI-H2030 cells harboring KRAS G12C mutant assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay
[PMID: 38232465]
In Vitro

MR-2088 (Compound 43) (0.005-5000 nM, 24 h) dose-dependently and specifically inhibits ULK1-mediated phosphorylation of the direct substrate ATG13 at Ser318, thereby preventing the degradation of autophagy markers p62 and LC3-II and effectively reversing starvation-induced activation of autophagic flux in H2030 cells[1].
MR-2088 (0-10 μM, 72 h) enhances the efficacy of Trametinib (HY-10999) (0-50 μM) by inhibiting ULK1/2 to block autophagy in H2030 cells (KRAS G12C mutant)[1].
MR-2088 inhibits enzymatic activity of ULK1 with a pIC50 value of 8.7 in HotSpot radioactive kinase assay and displays binding and enzymatic activity with a pIC50 value of 8.0 in NanoBRET assays in H2030 cells[1].
MR-2088 displays no significant inhibition of the hERG potassium channel (10 μM)[1].
MR-2088 (10 μM, 10 min) weakly inhibits CYP, including 1A2, 2C, 2D6, 3A4, CYP1A2, CYP2B6, CYP2C9, CYP2D6 and CYP3A4 with inhibition of 23%, 32%, 9%, 47%, 23.1%, 11.38%, 32.3%, 9.7%, 46.6%, respectively, in human liver microsomes[1].
MR-2088 displays good kinase selectivity inhibiting ULK2, ULK1, RET, AURKB, FLT3, ABL1 and CDK7 with pEC50 values of 8.7, 8.3, 6.7, 5.5, 5.3, <5 and <5, respectively, in NanoBRET assay[1].

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

MR-2088 Related Antibodies

Western Blot Analysis[1]

Cell Line: H2030 cells
Concentration: 0.005, 0.05, 0.5, 5, 50, 500 and 5000 nM
Incubation Time: 24 h
Result: Inhibited the phosphorylation of ATG13 Ser 318.
Prevented the degradation of p62.
Inhibited the phosphorylation of the direct substrate of ULK1 while preventing the degradation of p62 and LC3.

Cell Proliferation Assay[1]

Cell Line: H2030 cells (KRAS G12C mutant)
Concentration: 0, 0.5, 1.5, 4.5, 1.3, 4.0, 120, 360, 1200, 3400 and 10000 nM
Incubation Time: 72 h
Result: Observed potent antiproliferative synergy with the combination of Trametinib.
Inhibited H2030 cells (KRAS G12C mutant) antiproliferative activity with an IC50 value of 3.2 μM when not co-treated with Trametinib.
Strongly inhibited the proliferation of KRAS G12C-mutant H2030 cells when combination with Trametinib, with IC50 values of 196 µM (1:1), 3.6 µM (1:4), and 1.55 µM (4:1) for the respective molar ratios.
Parmacokinetics
Species Dose Route Cmax AUC T1/2 F
Mice[1] 1 nM i.v. 583 ng/mL 14900 min·ng/mL 1.1 h /
Mice[1] 10 nM p.o. 13.6 ng/mL 133. min·ng/mL 0.8 h <1 %
Mice[1] 20 nM i.p. 1667 ng/mL 345597 min·ng/mL 4.3 h /
Molecular Weight

406.42

Formula

C19H17F3N4OS
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(NCC(F)(F)F)C1=CC(C2=CN=C3C(C=C(C4=CCCNC4)N3)=C2)=CS1
Shipping

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

DMSO : 8.33 mg/mL (20.50 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 2.4605 mL 12.3025 mL 24.6051 mL
5 mM 0.4921 mL 2.4605 mL 4.9210 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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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 2.4605 mL 12.3025 mL 24.6051 mL 61.5127 mL
5 mM 0.4921 mL 2.4605 mL 4.9210 mL 12.3025 mL
10 mM 0.2461 mL 1.2303 mL 2.4605 mL 6.1513 mL
15 mM 0.1640 mL 0.8202 mL 1.6403 mL 4.1008 mL
20 mM 0.1230 mL 0.6151 mL 1.2303 mL 3.0756 mL
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MR-2088 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:

MR-20882922531-69-7MR2088MR 2088ULKAutophagyUnc-51 like kinaseH2030 cellsKRAS G12C mutantautophagic fluxnon-small lung cellInhibitorinhibitorinhibit

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