CLK1/2-IN-3

SKU: orb1703596

Description

CLK1/2-IN-3 is a selective inhibitor of CLK1 and CLK2 kinases, also affecting SRPK family members. It promotes nuclear speckle enlargement and induces selective splicing of S6K pre-mRNA, leading to antiproliferative effects in various cancer cell lines in vitro.

Research Area

Cell Biology, Metabolism Research, Signal Transduction

Key Properties

• CAS Number: 1005784-60-0
• MW: 375.42
• Purity: 99.04% (May vary between batches)
• Formula: C₂₁H₂₁N₅O₂
• SMILES: N(C(=O)C1=CC=C(C(CO)(C)C)C=C1)C2=CN3C(=N2)C=CC(=C3)C=4C=NNC4
• Target: Serine/threonin kinase,CDK
• Solubility: DMSO:3.76 mg/mL (10.02 mM)

Bioactivity

• Target IC50:
  SRPK3:260 nM|CLK1:1.1 nM|SRPK1:130 nM|SRPK2:260 nM|CLK2:2.1 nM
• In Vitro:
  Exposure to CLK1/2-IN-3 (compound 3) at concentrations of 1.1-3.3 μM for 72 hours increases the expression of S6K mRNAs in MDA-MB-468 cells. Significant reduction in the levels of endogenous phosphorylated SR proteins is observed with CLK1/2-IN-3 (5 μM).Anti-proliferative activity is demonstrated by CLK1/2-IN-3 (1-10 μM) with GI50s of 3.4, 2.6, 2.1, 2.5, 2.2, 2.9, 1.5 μM for MDA-MB-468, A549, COLO205, HCT-116, NCI-H23, SW620, COLO320DM cells,respectively.
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Storage & Handling

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

Alternative Names

CLK1/2IN3, CLK-1/2-IN-3, CLK1/2-IN-3, CLK1/2 inhibitor 3, CLK1/2-inhibitor-3, CLK2, CLK1/2 IN 3, CLK1

Compound Identifiers

PubChem CID

59175318