Cat. No.: HY-142812

GRK6-IN-1

4 Cited Publications

Customer Review

Based on 4 publication(s) in Google Scholar

GRK6-IN-1 (Compound 18) is the inhibitor for G protein-coupled receptorkinase 6 (GRK6) with an IC₅₀ of 3.8-8 nM. GRK6-IN-1 also inhibits GRK7, GRK5, GRK4 and GRK1 with IC₅₀s of 6.4, 12, 22 and 52 nM, respectively. GRK6-IN-1 has the potential for the research of multiple myeloma.

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

Purity: 99.61%
CAS No.: 2677786-61-5
Formula: C₂₂H₂₃ClN₆O₂
Molecular Weight:438.91

Storage:

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

GRK6-IN-1 Chemical Structure

CAS No.: 2677786-61-5

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (4)
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

GRK6

3.8-8 nM (IC₅₀)

GRK7

6.4 nM (IC₅₀)

GRK5

12 nM (IC₅₀)

GRK4

22 nM (IC₅₀)

GRK1

52 nM (IC₅₀)

Aurora A

8.9 μM (IC₅₀)

IGF-1R

9.2 μM (IC₅₀)

All Aurora Kinase Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
KMS-11	IC₅₀	0.34 μM Compound: 18	Antiproliferative activity against human KMS11 cells expressing pWPI assessed as reduction in cell viability incubated for 6 days by MTT assay Antiproliferative activity against human KMS11 cells expressing pWPI assessed as reduction in cell viability incubated for 6 days by MTT assay	[PMID: 34291633]
KMS-11	IC₅₀	0.44 μM Compound: 18	Antiproliferative activity against human KMS11 cells overexpressing pWPI-GRK6A assessed as reduction in cell viability incubated for 6 days by MTT assay Antiproliferative activity against human KMS11 cells overexpressing pWPI-GRK6A assessed as reduction in cell viability incubated for 6 days by MTT assay	[PMID: 34291633]
KMS-11	IC₅₀	1 μM Compound: 18	Antiproliferative activity against human KMS11 cells assessed as reduction in cell viability incubated for 3 days by MTT assay Antiproliferative activity against human KMS11 cells assessed as reduction in cell viability incubated for 3 days by MTT assay	[PMID: 34291633]
KMS-11	IC₅₀	1 μM Compound: 18	Antiproliferative activity against human KMS11 cells expressing pWPI assessed as reduction in cell viability incubated for 3 days by MTT assay Antiproliferative activity against human KMS11 cells expressing pWPI assessed as reduction in cell viability incubated for 3 days by MTT assay	[PMID: 34291633]
KMS-11	IC₅₀	1.1 μM Compound: 18	Antiproliferative activity against human KMS11 cells overexpressing pWPI-GRK6A assessed as reduction in cell viability incubated for 3 days by MTT assay Antiproliferative activity against human KMS11 cells overexpressing pWPI-GRK6A assessed as reduction in cell viability incubated for 3 days by MTT assay	[PMID: 34291633]
LP-1	IC₅₀	1.9 μM Compound: 18	Antiproliferative activity against human LP1 cells assessed as reduction in cell viability incubated for 3 days by MTT assay Antiproliferative activity against human LP1 cells assessed as reduction in cell viability incubated for 3 days by MTT assay	[PMID: 34291633]
RPMI-8226	IC₅₀	0.44 μM Compound: 18	Antiproliferative activity against human RPMI-8226 cells assessed as reduction in cell viability incubated for 6 days by MTT assay Antiproliferative activity against human RPMI-8226 cells assessed as reduction in cell viability incubated for 6 days by MTT assay	[PMID: 34291633]
RPMI-8226	IC₅₀	2.1 μM Compound: 18	Antiproliferative activity against human RPMI-8226 cells assessed as reduction in cell viability incubated for 3 days by MTT assay Antiproliferative activity against human RPMI-8226 cells assessed as reduction in cell viability incubated for 3 days by MTT assay	[PMID: 34291633]

In Vitro

GRK6-IN-1 inhibits Aurora A and IGF-1R with IC₅₀s of 8.9 μM and 9.2 μM^[1].
GRK6-IN-1 (1-10 μM, 3-6 days) inhibits the proliferation of multiple myeloma cells KMS11, KMS18, LP1, MM1R, RPMI-8226 with IC₅₀s of 1-3 μM (3 days incubation)^[1].
GRK6-IN-1 (50 μM, 30 min) affects the internalization and desensitization of oxytocin receptor in mouse primary neuronal cultures^[2].

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

Cell Proliferation Assay^[1]

Cell Line:

KMS11, KMS18, LP1, MM1R, RPMI-8226
Concentration:

1-10 μM
Incubation Time:

3-6 days
Result:

Inhibited the proliferation.

Chemical Information

CAS No. 2677786-61-5
Appearance Solid
Molecular Weight 438.91
Formula C₂₂H₂₃ClN₆O₂
Color White to off-white
SMILES

COC1=CC=CC2=NC(NCC3=CC=C(Cl)C=C3OC)=NC(NC4=NNC(CC)=C4)=C12
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Publications (4)

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Journal Impact Factor

Nat Commun

A heteromeric TRP channel that functions as a WNT-activated G protein-coupled receptor. [Abstract]

2026 Feb 26. PMID: 41748625
EMBO J

The global phosphorylation landscape of mouse oocytes during meiotic maturation. [Abstract]

2024 Oct;43(20):4752-4785. PMID: 39256562
Commun Biol

Cell-based and isoform-selective G protein-coupled receptor kinase assays for comprehensive inhibitor evaluation. [Abstract]

2026 Jan 16;9(1):287. PMID: 41545717
iScience

Robust GRK2/3/6-dependent desensitization of oxytocin receptor in neurons. [Abstract]

2024 May 22;27(6):110047. PMID: 38883814

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (113.92 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2784 mL

11.3919 mL

22.7837 mL

5 mM

0.4557 mL

2.2784 mL

4.5567 mL

10 mM

0.2278 mL

1.1392 mL

2.2784 mL

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.

Molarity Calculator

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

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Uehling DE, et al. Design, Synthesis, and Characterization of 4-Aminoquinazolines as Potent Inhibitors of the G Protein-Coupled Receptor Kinase 6 (GRK6) for the Treatment of Multiple Myeloma [published correction appears in J Med Chem. 2022 Jan 13;65(1):886-887]. J Med Chem. 2021;64(15):11129-11147. [Content Brief]

[2]. George K, et al., Robust GRK2/3/6-dependent desensitization of oxytocin receptor in neurons. iScience. 2024 May 22;27(6):110047. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	2.2784 mL	11.3919 mL	22.7837 mL	56.9593 mL
	5 mM	0.4557 mL	2.2784 mL	4.5567 mL	11.3919 mL
	10 mM	0.2278 mL	1.1392 mL	2.2784 mL	5.6959 mL
	15 mM	0.1519 mL	0.7595 mL	1.5189 mL	3.7973 mL
	20 mM	0.1139 mL	0.5696 mL	1.1392 mL	2.8480 mL
	25 mM	0.0911 mL	0.4557 mL	0.9113 mL	2.2784 mL
	30 mM	0.0759 mL	0.3797 mL	0.7595 mL	1.8986 mL
	40 mM	0.0570 mL	0.2848 mL	0.5696 mL	1.4240 mL
	50 mM	0.0456 mL	0.2278 mL	0.4557 mL	1.1392 mL
	60 mM	0.0380 mL	0.1899 mL	0.3797 mL	0.9493 mL
	80 mM	0.0285 mL	0.1424 mL	0.2848 mL	0.7120 mL
	100 mM	0.0228 mL	0.1139 mL	0.2278 mL	0.5696 mL

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GRK6-IN-1

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

GPCR/G Protein Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Cytoskeleton Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Angiogenesis-Related Compound Library

Anti-Prostate Cancer Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Cytokine Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) GRK6-IN-1

All Aurora Kinase Isoforms

Biological Activity

Chemical Information

Publications (4)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

GRK6-IN-1

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

GPCR/G Protein Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Cytoskeleton Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Angiogenesis-Related Compound Library

Anti-Prostate Cancer Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Cytokine Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) GRK6-IN-1

All Aurora Kinase Isoforms

Biological Activity

Chemical Information

Publications (4)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

GRK6-IN-1 Related Classifications

HY-142812 Related Classifications