HTH-01-091

SKU: orb1703371

Description

HTH-01-091 is a potent, selective MELK inhibitor (IC50 10.5 nM) with additional activity against kinases including PIM1-3 and RIPK2. This compound serves as a valuable chemical probe for studying MELK function in breast cancer research, enabling both in vitro and in vivo experimental investigations.

Research Area

Cell Biology, Epigenetics & Chromatin, Metabolism Research, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 2000209-42-5
• MW: 499.43
• Purity: 98.82% (May vary between batches)
• Formula: C₂₆H₂₈Cl₂N₄O₂
• SMILES: O=C1N(C2=C3C(=NC=C2CN1)C=CC(=C3)C4=CC(Cl)=C(O)C(Cl)=C4)[C@@H]5CC[C@@H](CN(C)C)CC5
• Target: mTOR,GSK-3,DYRK,RIP kinase,Serine/threonin kinase,CDK,MELK,Pim
• Solubility: DMSO:5 mg/mL (10.01 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2 mM)

Bioactivity

• Target IC50:
  DYRK4:41.8 nM|Pim1:60.6 nM|CDK7:1230 nM|mTOR:632 nM
• In Vitro:
  HTH-01-091 (0-10 μM, 1 h) 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 causes MELK degradation. HTH-01-091 (1 μM) selectively inhibits 4% of the kinases over 90%. HTH-01-091 (0-10 μM, 3 days) exhibits minor antiproliferative effects in breast cancer cells.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

DYRK, CLK2, MLCK, MELK, HTH 01091, HTH 01-091, HTH01091, HTH-01091, HTH-01-091, HTH01-091, Serine kinase, Serinekinase, threonin kinase, threoninkinase, Pim, RIP kinase, RIPkinase, RIPK2

Compound Identifiers

PubChem CID

131801426