GRK6-IN-1

Name: GRK6-IN-1
Brand: MedChemExpress
SKU: HY-142812
Rating: 5.0 (4 reviews)

Cat. No.: HY-142812 Purity: 99.61%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

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.

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GRK6-IN-1 화학구조

CAS No. : 2677786-61-5

사이즈	재고	수량

무료 샘플 (0.1 - 0.2 mg)	지금 신청하기
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	해외재고보유	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	해외재고보유	Estimated Time of Arrival: December 31
Solid
5 mg	해외재고보유	Estimated Time of Arrival: December 31
10 mg	해외재고보유	Estimated Time of Arrival: December 31
25 mg	해외재고보유	Estimated Time of Arrival: December 31
50 mg	해외재고보유	Estimated Time of Arrival: December 31
100 mg	해외재고보유	Estimated Time of Arrival: December 31
200 mg	견적 받기
500 mg	견적 받기

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고객리뷰

Based on 4 publication(s) in Google Scholar

4 Publications Citing Use of MCE GRK6-IN-1

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

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View All Aurora Kinase Isoform Specific Products:

View All Isoforms

Aurora Kinase Aurora A Aurora B Aurora C

Biological Activity
순도&문서
References
고객리뷰

제품 설명

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)

Cellular Effect

Cell Line	Type	Value	Description	References
KMS-11	IC₅₀	0.34 3 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	0.34 3 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	1 3 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	0.44 3 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	0.34 3 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 3 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 3 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 3 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	1.1 3 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]
KMS-11	IC₅₀	1 3 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 3 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	0.44 3 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	1.1 3 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]
KMS-11	IC₅₀	1.1 3 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 3 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]
LP-1	IC₅₀	1.9 3 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]
LP-1	IC₅₀	1.9 3 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	2.1 3 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]
RPMI-8226	IC₅₀	0.44 3 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	0.44 3 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	0.44 3 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 3 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]
RPMI-8226	IC₅₀	2.1 3 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.

분자량

438.91

화학식

C₂₂H₂₃ClN₆O₂

CAS No.

2677786-61-5

Appearance

Solid

Color

White to off-white

SMILES

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

선적

Room temperature in continental US; may vary elsewhere.

보관

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

용액&용해도

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

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.

몰농도 계산기
농도 희석 계산기

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

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In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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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

순도&문서

Purity: 99.61%

Select Batch:

Data Sheet (279 KB) SDS (393 KB)

COA (255 KB) HNMR (288 KB) LCMS (95 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]

Complete Stock Solution Preparation Table

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

GRK6-IN-1 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:

GRK6-IN-12677786-61-5G Protein-coupled Receptor Kinase (GRK)Aurora KinaseIGF-1RInsulin-like growth factor-1 receptorGRK6multiple myelomasurvivalInhibitorinhibitorinhibit

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GRK6-IN-1

고객리뷰

GRK6-IN-1 Related Antibodies

4 Publications Citing Use of MCE GRK6-IN-1

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Aurora Kinase Isoform Specific Products:

Biological Activity

순도&문서

References

고객리뷰

GRK6-IN-1 Related Antibodies

몰농도 계산기

농도 희석 계산기

Complete Stock Solution Preparation Table

GRK6-IN-1 Related Classifications

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고객리뷰

Request for HNMR Report

SAFETY DATA SHEET (SDS)

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