1. GPCR/G Protein
  2. G Protein-coupled Receptor Kinase (GRK)
  3. GRK6-IN-1

GRK6-IN-1 (compound 18) is a potent inhibitor of G protein-coupled receptor kinase 6 (GRK6) with an IC50 of 120 nM. GRK6 is a critical kinase required for the survival of multiple myeloma (MM) cells. GRK6-IN-1 has the potential for the research of multiple myeloma.

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

GRK6-IN-1 Chemical Structure

GRK6-IN-1 Chemical Structure

CAS No. : 2677786-61-5

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 165 In-stock
Solution
10 mM * 1 mL in DMSO USD 165 In-stock
Solid
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50 mg USD 950 In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

Top Publications Citing Use of Products

2 Publications Citing Use of MCE GRK6-IN-1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

GRK6-IN-1 (compound 18) is a potent inhibitor of G protein-coupled receptor kinase 6 (GRK6) with an IC50 of 120 nM. GRK6 is a critical kinase required for the survival of multiple myeloma (MM) cells. GRK6-IN-1 has the potential for the research of multiple myeloma[1].

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]
Molecular Weight

438.91

Formula

C22H23ClN6O2

CAS No.
Appearance

Solid

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
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)

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
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.

  • Molarity Calculator

  • Dilution Calculator

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

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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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
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 2.2784 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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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.

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Product Name:
GRK6-IN-1
Cat. No.:
HY-142812
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