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MedKoo Cat#: 555650 | Name: MELK-8a HCl
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

MELK-8a is a maternal embryonic leucine zipper kinase (MELK) inhibitor.

Chemical Structure

MELK-8a HCl
MELK-8a HCl
CAS# 2096992-20-8 (HCl)

Theoretical Analysis

MedKoo Cat#: 555650

Name: MELK-8a HCl

CAS#: 2096992-20-8 (HCl)

Chemical Formula: C25H33ClN6O

Exact Mass:

Molecular Weight: 469.03

Elemental Analysis: C, 64.02; H, 7.09; Cl, 7.56; N, 17.92; O, 3.41

Price and Availability

Size Price Availability Quantity
100mg USD 1,650.00 2 Weeks
200mg USD 2,850.00 2 Weeks
500mg USD 4,650.00 2 Weeks
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Related CAS #
2096992-20-8 (HCl) 1922153-17-0 (free base)
Synonym
MELK-8a HCl; MELK-8a HCl; MELK-8a HCl; MELK-8a hydrochloride
IUPAC/Chemical Name
1-methyl-4-(4-(4-(3-(piperidin-4-ylmethoxy)pyridin-4-yl)-1H-pyrazol-1-yl)phenyl)piperazine hydrochloride
InChi Key
AFGMSRRNYDSRPT-UHFFFAOYSA-N
InChi Code
InChI=1S/C25H32N6O.ClH/c1-29-12-14-30(15-13-29)22-2-4-23(5-3-22)31-18-21(16-28-31)24-8-11-27-17-25(24)32-19-20-6-9-26-10-7-20;/h2-5,8,11,16-18,20,26H,6-7,9-10,12-15,19H2,1H3;1H
SMILES Code
CN1CCN(C2=CC=C(N3N=CC(C4=C(OCC5CCNCC5)C=NC=C4)=C3)C=C2)CC1.[H]Cl
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
MELK-8a hydrochloride is a novel maternal embryonic leucine zipper kinase (MELK) inhibitor with an IC50 of 2 nM.
In vitro activity:
This study describes the discovery and optimization of novel MELK inhibitors 8a and 8b that recapitulate the cellular effects observed by short hairpin ribonucleic acid (shRNA)-mediated MELK knockdown in cellular models. Reference: J Med Chem. 2016 May 26;59(10):4711-23. https://pubmed.ncbi.nlm.nih.gov/27187609/
In vivo activity:
TBD
Solvent mg/mL mM
Solubility
DMSO 8.6 18.34
PBS (pH 7.2) 1.0 2.13
Water 100.0 213.21
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 469.03 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Sun H, Ma H, Zhang H, Ji M. Up-regulation of MELK by E2F1 promotes the proliferation in cervical cancer cells. Int J Biol Sci. 2021 Sep 7;17(14):3875-3888. doi: 10.7150/ijbs.62517. PMID: 34671205; PMCID: PMC8495384. 2. Touré BB, Giraldes J, Smith T, Sprague ER, Wang Y, Mathieu S, Chen Z, Mishina Y, Feng Y, Yan-Neale Y, Shakya S, Chen D, Meyer M, Puleo D, Brazell JT, Straub C, Sage D, Wright K, Yuan Y, Chen X, Duca J, Kim S, Tian L, Martin E, Hurov K, Shao W. 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. doi: 10.1021/acs.jmedchem.6b00052. Epub 2016 May 17. PMID: 27187609.
In vitro protocol:
1. Sun H, Ma H, Zhang H, Ji M. Up-regulation of MELK by E2F1 promotes the proliferation in cervical cancer cells. Int J Biol Sci. 2021 Sep 7;17(14):3875-3888. doi: 10.7150/ijbs.62517. PMID: 34671205; PMCID: PMC8495384. 2. Touré BB, Giraldes J, Smith T, Sprague ER, Wang Y, Mathieu S, Chen Z, Mishina Y, Feng Y, Yan-Neale Y, Shakya S, Chen D, Meyer M, Puleo D, Brazell JT, Straub C, Sage D, Wright K, Yuan Y, Chen X, Duca J, Kim S, Tian L, Martin E, Hurov K, Shao W. 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. doi: 10.1021/acs.jmedchem.6b00052. Epub 2016 May 17. PMID: 27187609.
In vivo protocol:
TBD