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532604 MELK Inhibitor, OTSSP167 - Calbiochem

MELK Inhibitor, OTSSP167 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: Maternal Embryonic Leucine Zipper Kinase Inhibitor

Primary Target: MELK
532604
  
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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₂₅H₃₀Cl₄N₄O₂
Description
Overview

This product has been discontinued.



A cell permeable, orally bioavailable 1, 5-naphthyridine based compound that acts as a highly potent and specific inhibitor of maternal embryonic leucine zipper kinase (MELK; IC50 = 410 pM). Inhibits mammospheres formation of MDA-MB-231 and MCF-7 cells by blocking MELK-dependent phosphorylation of proteasome subunit a1 (PSMA1). Also diminishes the phosphorylation of Ser269 on drebin-like (DBNL) in BT549 cells and reduces their invasiveness. Suppresses the growth of xenografted MDA-MD-231 cells in a murine model (20 mg/kg, once every 2 days for 14 days, i.v). Induces the formation of autophagosome-like vesicles in cytoplasm of BT549 breast cancer cells. Also shown to suppress the growth of lung, pancreatic, and prostate cancer cells expressing high levels of MELK.

Please note that the molecular weight for this compound is batch-specific due to variable water content.
Catalogue Number532604
Brand Family Calbiochem®
SynonymsMaternal Embryonic Leucine Zipper Kinase Inhibitor
References
ReferencesChung, S., et al. 2013. Cell Cycle. 12, 1655.
Product Information
FormBeige powder
Hill FormulaC₂₅H₃₀Cl₄N₄O₂
Chemical formulaC₂₅H₃₀Cl₄N₄O₂
ReversibleY
Quality LevelMQ100
Applications
Biological Information
Primary TargetMELK
Primary Target IC<sub>50</sub>410 pM
Purity≥98% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Toxicity Standard Handling
Storage -20°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalogue Number GTIN
532604 0

Documentation

MELK Inhibitor, OTSSP167 - Calbiochem MSDS

Title

Safety Data Sheet (SDS) 

References

Reference overview
Chung, S., et al. 2013. Cell Cycle. 12, 1655.

Brochure

Title
NPI Flyer- Epigenetics and Nuclear Function Feature
New Products - Antibodies, Small Molecule, Inhibitors

Technical Info

Title
White Paper: Further considerations of antibody validation and usage.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision19-December-2014 JSW
SynonymsMaternal Embryonic Leucine Zipper Kinase Inhibitor
DescriptionA cell permeable, orally bioavailable 1, 5-naphthyridine based compound that acts as a highly potent and specific inhibitor of maternal embryonic leucine zipper kinase (MELK; IC50 = 410 pM). Inhibits mammospheres formation of MDA-MB-231 and MCF-7 cells by blocking MELK-dependent phosphorylation of proteasome subunit a1 (PSMA1). Also diminishes the phosphorylation of Ser269 on drebin-like (DBNL) in BT549 cells and reduces their invasiveness. Suppresses the growth of xenografted MDA-MD-231 cells in a murine model (20 mg/kg, once every 2 days for 14 days, i.v). Induces the formation of autophagosome-like vesicles in cytoplasm of BT549 breast cancer cells. Also shown to suppress the growth of lung, pancreatic, and prostate cancer cells expressing high levels of MELK.
FormBeige powder
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₂₅H₃₀Cl₄N₄O₂
Purity≥98% by HPLC
SolubilityDMSO (50 mg/ml) or H₂O (5 mg/ml)
Storage Protect from light
-20°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesChung, S., et al. 2013. Cell Cycle. 12, 1655.