GRK6-IN-1
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.
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- 純度: 99.61%
- CAS 番号: 2677786-61-5
- 分子式: C22H23ClN6O2
- 分子量:438.91
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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溶剤 & 溶解度
- 純度とドキュメンテーション
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MedChemExpress（MCE）の使用を引用している文献 GRK6-IN-1
MoreAurora Kinase アイソフォーム固有の製品をすべて表示
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生物活性
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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) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| KMS-11 | IC50 |
0.34 μM
Compound: 18
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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
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[PMID: 34291633] |
| KMS-11 | IC50 |
0.44 μM
Compound: 18
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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
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[PMID: 34291633] |
| KMS-11 | IC50 |
1 μM
Compound: 18
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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
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[PMID: 34291633] |
| KMS-11 | IC50 |
1 μM
Compound: 18
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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
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[PMID: 34291633] |
| KMS-11 | IC50 |
1.1 μM
Compound: 18
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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
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[PMID: 34291633] |
| LP-1 | IC50 |
1.9 μM
Compound: 18
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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
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[PMID: 34291633] |
| RPMI-8226 | IC50 |
0.44 μM
Compound: 18
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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
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[PMID: 34291633] |
| RPMI-8226 | IC50 |
2.1 μM
Compound: 18
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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] |
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.
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Cell Line:KMS11, KMS18, LP1, MM1R, RPMI-8226
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Concentration:1-10 μM
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Incubation Time:3-6 days
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Result:Inhibited the proliferation.
化学情報
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CAS 番号 2677786-61-5
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性状 Solid
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分子量 438.91
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分子式 C22H23ClN6O2
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Color White to off-white
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SMILES
COC1=CC=CC2=NC(NCC3=CC=C(Cl)C=C3OC)=NC(NC4=NNC(CC)=C4)=C12
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
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
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Most Recent
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Nat Commun
2026 Feb 26. PMID: 41748625 -
EMBO J
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
2024 May 22;27(6):110047. PMID: 38883814
溶剤 & 溶解度
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)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (279 KB)
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SDS (393 KB)
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- Deutsch - DE (393 KB)
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取扱説明書 (2659 KB)
参考文献
[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
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 |
GRK6-IN-1 関連分類
HY-142812 関連分類
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