HTH-01-091 , CAS No.2000209-42-5

CAS: 2000209-42-5 Cat. No.: H650200 Summenformel: C₂₆H₂₈Cl₂N₄O₂ Molekulargewicht: 499.43

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

Übersicht

HTH-01-091 is a potent and selective maternal embryonic leucine zipper kinase (MELK) inhibitor, with an IC 50 of 10.5 nM. HTH-01-091 also inhibits PIM1/2/3 , RIPK2 , DYRK3 , smMLCK and CLK2 . HTH-01-091 can be uesd for breast cancer research

In Vitro

HTH-01-091 (1 μM) selectively inhibits 4% of the kinases over 90%. HTH-01-091 (0-10 μM, 1 h) is cell permeable and causes MELK degradation. HTH-01-091 (0-10 μM, 3 day) exhibits minor antiproliferative effects in breast cancer cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: MDA-MB-468 cells Concentration: 0, 0.1, 1.0, and 10 μM Incubation Time: 1 h Result: Reduced MELK protein levels in MDA-MB-468 cells; Dose-dependently decreased MELK pull-down by streptavidin beads, demonstrating that the compound is cell permeable and binds to MELK in an ATP-competitive fashion. Had no effect on ERK1/2 pull-down, showing no binding affinity of HTH-01-091 to ERK1/2. Cell Proliferation AssayCell Line: MDA-MB-468, BT-549, HCC70, ZR-75-1, MCF7, and T-47D cells Concentration: 0, 0.001, 0.01, 0.1, 1.0, and 10 μM Incubation Time: 3 day Result: Showed antiproliferative activities in a panel of breast cancer cell lines, including MDA-MB-468, BT-549, HCC70, ZR-75-1, MCF7, and T-47D cells, with IC 50 values of 4.00 μM, 6.16 μM, 8.80 μM, >10 μM, 8.75 μM, and 3.87 μM, respectively.

IC50& Target:DYRK4 41.8 nM (IC 50 ) PIM1 60.6 nM (IC 50 ) mTOR 632 nM (IC 50 ) CDK7 1230 nM (IC 50 ) PIM2 PIM3

Specifications

Biochemische und physiologische Mechanismen

HTH-01-091 is a potent and selective maternal embryonic leucine zipper kinase (MELK) inhibitor, with an IC 50 of 10.5 nM. HTH-01-091 also inhibits PIM1/2/3 , RIPK2 , DYRK3 , smMLCK and CLK2 . HTH-01-091 can be uesd for breast cancer research.

Storage

Store at -20°C

Verschickt in

Ice chest + Ice pads

Dieses Produkt erfordert Kühlkettenversand. Grundversand und andere Economy-Optionen sind nicht verfügbar.

Aktionsart

INHIBITOR

Namen und Kennungen

Molekulargewicht

499.43

Häufig gestellte Fragen

How should this product be stored?

Store at ?20 °C. Freezer storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships in an insulated container with ice pads. Unpack on arrival and transfer it to the storage condition stated above.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 2000209-42-5, the molecular formula is C26H28Cl2N4O2, and the molecular weight is 499.43 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.