製品番号: HY-117548

UNC1062

2 Cited Publications

カスタマーレビュー

Based on 2 publication(s) in Google Scholar

UNC1062 is a highly selective tyrosine kinase (MERTK) inhibitor with an IC₅₀ of 1.1 nM (Morrison K_i = 0.33 nM). UNC1062 exhibits good selectivity for the TAM family (TYRO3 IC₅₀ = 60 nM, AXL IC₅₀ = 85 nM). UNC1062 exhibits significant anti-proliferative effects and induces apoptosis in various cancer models (such as melanoma, gastric cancer, and acute myeloid leukemia). UNC1062 inhibits multiple pathways, including MAPK/ERK, PI3K/AKT and JAK/STAT and affects the motility of head and neck squamous cell carcinoma (HNSCC) cells through the RhoA signaling pathway. UNC1062 inhibits macrophage efferocytosis, and it suitable for research on atherosclerosis.

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純度: 98.92%
CAS 番号: 1350549-36-8
分子式: C₂₅H₃₄N₆O₄S
分子量:514.64

保管条件:

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

UNC1062 構造式

CAS 番号: 1350549-36-8

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数量

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Use of MCE Products

Fluorescent Dye

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

生物活性

製品説明

IC₅₀ & Target^[1]

Axl

85 nM ()

Tyro3

60 nM ()

STAT6

Akt

ERK1

ERK2

TAM Receptor アイソフォーム固有の製品をすべて表示 :

p38 MAPK アイソフォーム固有の製品をすべて表示 :

ERK アイソフォーム固有の製品をすべて表示 :

PI3K アイソフォーム固有の製品をすべて表示 :

Akt アイソフォーム固有の製品をすべて表示 :

JAK アイソフォーム固有の製品をすべて表示 :

STAT アイソフォーム固有の製品をすべて表示 :

体外実験

UNC1062 (0.5-10 μM, 72 h-21 d) inhibits acute myeloid leukemia (AML) cell lines (OCI/AML5, TMD7, THP-1 and HEL cells) and gastric cancer cell lines (HSC-60 and SNU-5) proliferation and inhibits melanoma cell lines (HMCB and G361 cells) and gastric cancer cells colony formation^[1]^[2]^[3].
UNC1062 (0.5-2 μM, 48 h) induces apoptosis of melanoma cell lines (HMCB and G361 cells), AML cell lines (OCI/AML5, TMD7, THP-1 and HEL cells) and gastric cancer cell lines (HSC-60 and SNU-5)^[1]^[2]^[3].
UNC1062 (1-5 μM, 24-72 h) causes G2 arrest in gastric cancer cell lines and HNSCC cell lines (G2 arrest cells and NC cells)^[3]^[4].
UNC1062 (0.25-1 μM, 16-96 h) significantly weakens the migration and invasion ability of SKMEL119 cells and Detroit 562 cells^[1]^[4].
UNC1062 (0.1-2 μM, 90-100 min) inhibits MERTK phosphorylation and significantly attenuates GAS6-induced activation of STAT6, AKT, and ERK1/2^[1].
UNC1062 (20 μg/L, 18.5 h) attenuates the effects of Ru360 (a mitochondrial calcium uniporter (MCU) inhibitor) in reducing inflammatory cytokines and intracytoplasmic lipid content in primary mouse macrophages, it was confirmed that MCU affects inflammatory response by regulating efferocytosis^[5].

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

Apoptosis Analysis^[1]^[2]

Cell Line:

Melanoma cell lines (HMCB and G361 cells) and AML cell lines (OCI/AML5, TMD7, THP-1 and HEL cells)
Concentration:

0.5 and 1 μM for melanoma cell lines and 2 μM for AML cell lines
Incubation Time:

48 h
Result:

Increased cell death rate and PARP cleavage (caspase-3).

Cell Migration Assay ^[1]^[4]

Cell Line:

SKMEL119 cells and Detroit 562 cells
Concentration:

1 μM for SKMEL119 cells and 0.25 μM for Detroit 562 cells
Incubation Time:

16 h for SKMEL119 cells and 24 h Detroit 562 cells
Result:

Exhibited significant 30% decrease in the velocity of individual SKMEL119 cell migration.
Exhibited an 40% reduction in invasion in Detroit 562 cells.

Cell Migration Assay ^[1]^[4]

Cell Line:

SKMEL119 cells and Detroit 562 cells
Concentration:

1 μM for SKMEL119 cells and 0.25 μM for Detroit 562 cells
Incubation Time:

96 h for SKMEL119 cells and 24 h Detroit 562 cells
Result:

Exhibited an 89% reduction in invasion in SKMEL119 cells.
Exhibited an 45% reduction in invasion in Detroit 562 cells.

Western Blot Analysis^[1]

Cell Line:

HMCB and G361 cells
Concentration:

0.1, 0.2, 0.5, 1 and 2 μM
Incubation Time:

After 90 min of pre-treatment, add GAS6 (HY-P75174) for 10 min
Result:

Dose-dependently reduced MERTK phosphorylation.
Significantly attenuated GAS6-induced activation of STAT6, AKT, and ERK1/2.

化学情報

CAS 番号 1350549-36-8
性状 Solid
分子量 514.64
分子式 C₂₅H₃₄N₆O₄S
Color White to off-white
SMILES

O[C@H]1CC[C@H](N2N=C(C3=CC=C(S(=O)(N4CCOCC4)=O)C=C3)C5=CN=C(NCCCC)N=C52)CC1
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

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

Publications (2)

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Immunol Lett

Modulation of Oxidized Low-density Lipoprotein-Affected Macrophage Efferocytosis by Mitochondrial Calcium Uniporter in a Murine Model. [Abstract]

2023 Nov:263:14-24. PMID: 37689315
Res Sq

2025 Mar 30.

溶剤 & 溶解度

体外:

DMSO : 10 mg/mL (19.43 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)

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

1.9431 mL

9.7155 mL

19.4311 mL

5 mM

0.3886 mL

1.9431 mL

3.8862 mL

10 mM

0.1943 mL

0.9716 mL

1.9431 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.

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (282 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
元素分析報告書 (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)
取扱説明書 (2659 KB)

参考文献

[1]. Schlegel J, et al. MERTK receptor tyrosine kinase is a therapeutic target in melanoma. J Clin Invest. 2013;123(5):2257-2267. [Content Brief]

[2]. Koda Y, Itoh M, Tohda S. Effects of MERTK Inhibitors UNC569 and UNC1062 on the Growth of Acute Myeloid Leukaemia Cells. Anticancer Res. 2018 Jan;38(1):199-204. [Content Brief]

[3]. Yi JH, et al. MerTK is a novel therapeutic target in gastric cancer. Oncotarget. 2015 Apr 20;8(57):96656-96667. [Content Brief]

[4]. von Mässenhausen A, et al. MERTK as a novel therapeutic target in head and neck cancer. Oncotarget. 2016 May 31;7(22):32678-94. [Content Brief]

[5]. Lu N, et al. Modulation of oxidized low-density lipoprotein-affected macrophage efferocytosis by mitochondrial calcium uniporter in a murine model. Immunol Lett. 2023 Nov;263:14-24. [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	1.9431 mL	9.7155 mL	19.4311 mL	48.5776 mL
	5 mM	0.3886 mL	1.9431 mL	3.8862 mL	9.7155 mL
	10 mM	0.1943 mL	0.9716 mL	1.9431 mL	4.8578 mL
	15 mM	0.1295 mL	0.6477 mL	1.2954 mL	3.2385 mL

UNC1062

2 Cited Publications

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UNC1062

Apoptosis Compound Library

Epigenetics Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

MAPK Compound Library

PI3K/Akt/mTOR Compound Library

Protein Tyrosine Kinase Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Anti-Cardiovascular Disease Compound Library

Glycolysis Compound Library

Pyroptosis Compound Library

Cytoskeleton Compound Library

Glutamine Metabolism Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Neurodegenerative Disease-related Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Transcription Factor-Targeted Library

Glucose Metabolism Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Antidepressant Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Autoimmune Disease Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Macrophage Related Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

Lactylation Compound Library

MedChemExpress（MCE）の使用を引用している文献 UNC1062

TAM Receptor アイソフォーム固有の製品をすべて表示

p38 MAPK アイソフォーム固有の製品をすべて表示

ERK アイソフォーム固有の製品をすべて表示

PI3K アイソフォーム固有の製品をすべて表示

Akt アイソフォーム固有の製品をすべて表示

JAK アイソフォーム固有の製品をすべて表示

STAT アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (2)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

UNC1062 関連分類