2. Protein Tyrosine Kinase/RTK Apoptosis MAPK/ERK Pathway Stem Cell/Wnt PI3K/Akt/mTOR JAK/STAT Signaling Epigenetics
  3. TAM Receptor Apoptosis p38 MAPK ERK PI3K Akt JAK STAT
  4. UNC1062

UNC1062 is a highly selective tyrosine kinase (MERTK) inhibitor with an IC50 of 1.1 nM (Morrison Ki = 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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UNC1062

UNC1062 構造式

CAS 番号 : 1350549-36-8

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 396 在庫あり
Solution
10 mM * 1 mL in DMSO USD 396 在庫あり
Solid
1 mg $175 在庫あり
5 mg $350 在庫あり
10 mg $462 在庫あり
25 mg $833 在庫あり
50 mg $1325 在庫あり
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Based on 2 publication(s) in Google Scholar

UNC1062 関連抗体

Top Publications Citing Use of Products

TAM Receptor アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
Axl Mer Tyro3

p38 MAPK アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
p38 MAPK Akt1 p38α p38β MAPK13 p38δ p38γ

ERK アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
ERK ERK1 ERK2 ERK5 ERK8

PI3K アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

Akt アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
Akt Akt1 Akt2 Akt3

JAK アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
JAK1 JAK2 JAK3 Tyk2 JAK

STAT アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
STAT3 STAT5 STAT6 STAT1

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製品説明

UNC1062 is a highly selective tyrosine kinase (MERTK) inhibitor with an IC50 of 1.1 nM (Morrison Ki = 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[1][2][3][4][5].

IC50 & Target[1]

Axl

85 nM ()

Tyro3

60 nM ()

STAT6

 

Akt

 

ERK1

 

ERK2

 

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.

UNC1062 関連抗体

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.
分子量

514.64

分子式

C25H34N6O4S
CAS 番号
Appearance

Solid

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
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
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
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.

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純度とドキュメンテーション
参考文献

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 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
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UNC1062 Related Classifications

  • Molarity Calculator

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The molarity calculator equation

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

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The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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:

UNC10621350549-36-8UNC 1062UNC-1062TAM ReceptorApoptosisp38 MAPKERKPI3KAktJAKSTATTyro3AxlMerExtracellular signal regulated kinasesPhosphoinositide 3-kinasePKBProtein kinase BJanus kinaseLeukaemiaGastric cancerMerTKPatient-derived cellsAtherosclerosisEfferocytosisMacrophageMCUox-LDLInhibitorinhibitorinhibit

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