Referencia número: HY-100368A

MELK-8a hydrochloride

Name: MELK-8a hydrochloride
Brand: MedChemExpress
SKU: HY-100368A
Price: 100.00 USD
Availability: InStock
Rating: 5 (3 reviews)

(Synonyms: NVS-MELK8a hydrochloride)

3 Cited Publications

Revisión del cliente

Based on 3 publication(s) in Google Scholar

MELK-8a hydrochloride is a novel maternal embryonic leucine zipper kinase (MELK) inhibitor with an IC₅₀ of 2 nM.

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Pureza : 99.31%
No. CAS: 2096992-20-8
Fòrmula: C₂₅H₃₃ClN₆O
Peso molecular:469.02

Almacenamiento:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

MELK-8a hydrochloride Chemical Structure

No. CAS: 2096992-20-8

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Actividad biológica
- Descripciòn
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (3)
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

MELK-8a hydrochloride is a novel maternal embryonic leucine zipper kinase (MELK) inhibitor with an IC₅₀ of 2 nM.

IC₅₀ & Target

IC50: 2 nM (MELK)^[1]

In Vitro

MELK-8a remains very potent (IC₅₀=140 nM) when the ATP concentration in the biochemical assay is shifted from 20 μM to 2 mM. Its potency is well tracked between full-length MELK versus catalytic domain construct (5 nM versus 2 nM). It only inhibits seven off-target kinases in addition to MELK with >85% inhibition of binding at 1 μM demonstrating great selectivity. The compound is at least 90-fold more selective in targeting MELK in all cases. MELK-8a is fairly soluble (0.22 g/L at pH 6.8) and shows a good permeability in the Caco-2 assay. MELK-8a inhibits the growth of MDA-MB-468 cells and MCF-7 cells with an IC₅₀ of approximately 0.06 and 1.2 μM, respectively^[1].

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

In Vivo

Subcutaneous administration of MELK-8a at 30 mg/kg in C57BL/6 mice results in good plasma exposure. The compound adsorption into the systemic circulation is rapid (T_max=0.4 h) and peak plasma concentration reaches 6.6 μM. An ascending dose PK study in female athymic nude mice shows that the rate of compound release is maximal at 120 mg/kg and all clearance mechanisms can be saturated at 240 mg/kg. However, when administered orally at 10 mg/kg in C57BL/6 male mice, it shows very poor PK (3.6% oral bioavailability) consistent with very high in vivo clearance^[1].

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

Chemical Information

No. CAS 2096992-20-8
Appearance Solid
Peso molecular 469.02
Fòrmula C₂₅H₃₃ClN₆O
Color Light yellow to yellow
SMILES

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

NVS-MELK8a hydrochloride
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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 hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride 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.

Solvente y solubilidad

In Vitro:

H₂O : ≥ 100 mg/mL (213.21 mM)

DMSO : 8.6 mg/mL (18.34 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

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

2.1321 mL

10.6605 mL

21.3211 mL

5 mM

0.4264 mL

2.1321 mL

4.2642 mL

10 mM

0.2132 mL

1.0661 mL

2.1321 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS

Solubility: 50 mg/mL (106.61 mM); Clear solution; Need ultrasonic

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (278 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Touré BB, 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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO / H₂O	1 mM	2.1321 mL	10.6605 mL	21.3211 mL	53.3026 mL
	5 mM	0.4264 mL	2.1321 mL	4.2642 mL	10.6605 mL
	10 mM	0.2132 mL	1.0661 mL	2.1321 mL	5.3303 mL
	15 mM	0.1421 mL	0.7107 mL	1.4214 mL	3.5535 mL
H₂O	20 mM	0.1066 mL	0.5330 mL	1.0661 mL	2.6651 mL
	25 mM	0.0853 mL	0.4264 mL	0.8528 mL	2.1321 mL
	30 mM	0.0711 mL	0.3554 mL	0.7107 mL	1.7768 mL
	40 mM	0.0533 mL	0.2665 mL	0.5330 mL	1.3326 mL
	50 mM	0.0426 mL	0.2132 mL	0.4264 mL	1.0661 mL
	60 mM	0.0355 mL	0.1777 mL	0.3554 mL	0.8884 mL
	80 mM	0.0267 mL	0.1333 mL	0.2665 mL	0.6663 mL
	100 mM	0.0213 mL	0.1066 mL	0.2132 mL	0.5330 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Bioz

Keywords

MELK-8a hydrochloride

3 Cited Publications

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MELK-8a hydrochloride

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