Cat. No.: HY-100368

MELK-8a

Name: MELK-8a
Brand: MedChemExpress
SKU: HY-100368
Price: 90.00 USD
Availability: InStock
Rating: 5 (3 reviews)

(Synonyms: NVS-MELK8a)

3 Cited Publications

고객리뷰

Based on 3 publication(s) in Google Scholar

MELK-8a (NVS-MELK8a) is a highly potent and selective maternal embryonic leucine zipper kinase (MELK) inhibitor with IC₅₀ of 2 nM. MELK-8a also inhibits Flt3 (ITD), Haspin, PDGFRα with IC₅₀s of 0.18, 0.19, and 0.42 μM, respectively. MELK plays an essential role in regulating cell mitosis in a subset of cancer cells.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

Purity: 98.32%
CAS No.: 1922153-17-0
화학식: C₂₅H₃₂N₆O
분자량:432.56

보관:

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

MELK-8a Chemical Structure

CAS No.: 1922153-17-0

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biological Activity
- 제품 설명
- Cellular Effect
Chemical Information
Publications (3)
용액&용해도
- In Vitro
순도&문서
References
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

All PDGFR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
MCF7	IC₅₀	3.68 μM Compound: 8a	Antiproliferative activity against MELK-independent ER-positive human MCF7 cells assessed as reduction in cell viability after 7 days by CellTiter-Glo assay Antiproliferative activity against MELK-independent ER-positive human MCF7 cells assessed as reduction in cell viability after 7 days by CellTiter-Glo assay	[PMID: 27187609]
MDA-MB-231	CC₅₀	2.3 μM Compound: MELK-8a	Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 72 to 96 hrs by CCK-8 method Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 72 to 96 hrs by CCK-8 method	[PMID: 39026635]
MDA-MB-468	IC₅₀	0.11 μM Compound: 8a	Antiproliferative activity against MELK-dependent human MDA-MB-468 cells assessed as reduction in cell viability after 7 days by CellTiter-Glo assay Antiproliferative activity against MELK-dependent human MDA-MB-468 cells assessed as reduction in cell viability after 7 days by CellTiter-Glo assay	[PMID: 27187609]
Ramos	IC₅₀	3.4 μM Compound: MELK-8a	Cytotoxicity against human Ramos cells assessed as inhibition of cell growth measured after 72 to 96 hrs by CCK-8 method Cytotoxicity against human Ramos cells assessed as inhibition of cell growth measured after 72 to 96 hrs by CCK-8 method	[PMID: 39026635]

Chemical Information

CAS No. 1922153-17-0
Appearance Solid
분자량 432.56
화학식 C₂₅H₃₂N₆O
Color Off-white to light yellow
SMILES

CN(CC1)CCN1C2=CC=C(N3C=C(C4=CC=NC=C4OCC5CCNCC5)C=N3)C=C2
Synonyms

NVS-MELK8a
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

Publications (3)

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Cell Rep

MELK Promotes Melanoma Growth by Stimulating the NF-κB Pathway. [Abstract]

2017 Dec 5;21(10):2829-2841. PMID: 29212029

MELK-8a purchased from MedChemExpress. Usage Cited in: Cell Rep. 2017 Dec 5;21(10):2829-2841. [Abstract]

A375 cells are treated with MELK-8a for 48 h and analyzed for indicated proteins by immunoblot analysis. ACTINB is used for as a loading control.
J Biol Chem

Mass spectrometry-based selectivity profiling identifies a highly selective inhibitor of the kinase MELK that delays mitotic entry in cancer cells. [Abstract]

2020 Feb 21;295(8):2359-2374. PMID: 31896573

MELK-8a purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2020 Feb 21;295(8):2359-2374. [Abstract]

HeLaS3 cells treated with 8a complete mitosis and begin the subsequent cell cycle following delayed mitotic entry. HeLaS3 cells are synchronized at G1/S with double thymidine block and released into DMSO or 3 μM 8a. Cells are collected starting at 6h post-release, with subsequent collections completed every 2h over a 20h timecourse. Cells are lysed and immunoblotted with the indicated antibodies. The split in the image indicates that the samples from DMSO and 3 μM 8a conditions are blotted sepa

MELK-8a purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2020 Feb 21;295(8):2359-2374. [Abstract]

Delayed mitotic entry caused by 8a is associated with delayed activation of Aurora A, Aurora B, and CDK1. HeLaS3 cells are synchronized at G1/S with double thymidine block and released into DMSO or 3 μM 8a. Cells are collected starting at 6h post-release, with subsequent collections completed every 0.5 or 1h, over a 12h timecourse. Cells are lysed and immunoblotted with the indicated antibodies. The split in the image indicates that the samples from DMSO and 3 μM 8a conditions are blotted sepa.

MELK-8a purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2020 Feb 21;295(8):2359-2374. [Abstract]

MELK inhibition with 3 μM 8a causes delayed mitotic entry. HeLaS3 cells are synchronized at G1/S with double thymidine block and released into DMSO, 1 μM, or 3 μM 8a. Cells are collected every 2h over a 12h timecourse. Cells are lysed and immunoblotted with the indicated antibodies. The splits in the image indicate that the samples from DMSO, 1 μM, and 3 μM 8a conditions are immunoblotted separately due to space constraints. Asynchronous HeLaS3 lysate is loaded in the lanes labeled “A” in order

MELK-8a purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2020 Feb 21;295(8):2359-2374. [Abstract]

Asynchronous MDA-MB-468 cells are treated with DMSO or 0.5, 1, or 3 μM 8a for 1, 6, or 24h. Cells are harvested and immunoblotted with the indicated antibodies.
University of North Carolina at Chapel Hill

2020 Jun.

용액&용해도

In Vitro:

DMSO : 10 mg/mL (23.12 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

2.3118 mL

11.5591 mL

23.1182 mL

5 mM

0.4624 mL

2.3118 mL

4.6236 mL

10 mM

0.2312 mL

1.1559 mL

2.3118 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.

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 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)
Elemental Analysis Report (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)
Handling Instructions (2659 KB)

References

[1]. B Barry Touré, et al. Toward the Validation of Maternal Embryonic Leucine Zipper Kinase: Discovery, Optimization of Highly Potent and Selective Inhibitors, and Preliminary Biology Insight. J Med Chem. 2016 May 26;59(10):4711-23. [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	2.3118 mL	11.5591 mL	23.1182 mL	57.7955 mL
	5 mM	0.4624 mL	2.3118 mL	4.6236 mL	11.5591 mL
	10 mM	0.2312 mL	1.1559 mL	2.3118 mL	5.7795 mL
	15 mM	0.1541 mL	0.7706 mL	1.5412 mL	3.8530 mL
	20 mM	0.1156 mL	0.5780 mL	1.1559 mL	2.8898 mL

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MELK-8a

Publications Citing Use of MedChemExpress (MCE) MELK-8a

All PDGFR Isoforms