Longdaysin

SKU: orb1301856

Description

Longdaysin

Research Area

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

Key Properties

• CAS Number: 1353867-91-0
• MW: 335.33
• Purity: 99.97%
• Formula: C₁₆H₁₆F₃N₅
• SMILES: CC(C)n1cnc2c(NCc3cccc(c3)C(F)(F)F)ncnc12
• Target: ERK,Wnt/beta-catenin,Casein Kinase,CDK
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (11.93 mM);H2O:Insoluble;DMSO:100 mg/mL (298.21 mM)

Bioactivity

• Target IC50:
  CKIδ:8.8 μM (cell free)|ERK2:52 μM (cell free)|CKIα:5.6 μM (cell free)|CDK7:29 μM (cell free)
• In Vivo:
  In MDA-MB-231 breast cancer xenografts, treatment with longdaysin suppressed tumor growth in association with inhibition of Wnt/β-catenin signaling .
• In Vitro:
  Longdaysin inhibited CKIδ, CKIα, ERK2, and CDK7 activities (IC50 = 8.8, 5.6, 52, and 29 μM, respectively), while it had much less effect on p38α. The period of CKIδ deficient cells was 1.1 h longer than that of wild type cells. Longdaysin lengthened the period in a dose-dependent manner in CKIδ deficient cells as well as in wild type cells . In breast cancer Hs578T and MDA-MB-231 cells, micromolar concentrations of longdaysin attenuated the phosphorylation of LRP6 and DVL2 and reduced the expression of active β-catenin and total β-catenin, leading to the downregulation of Wnt target genes Axin2, DKK1, LEF1, and Survivin .
• Cell Research:
  2×10^5 cells were suspended in 100 μL serum-free medium containing the indicated concentrations of longdaysin, and then seeded in 24-transwell chambers with 8 μm pore membrane. The lower chamber contained medium with 20% FBS. After incubation at 37°C for 6 hours, the unmigrated cells on the upper side of membrane were removed by a cotton swab, and the migrated cells were stained with crystal violet and stained cells were photomicrographed. For invasion assays, the transwell chambers with 8 μm pore membranes were coated with Matrigel .
• Animal Research:
  MDA-MB-231 cells were injected s.c. into the right flank of nude mice (1×10^7 cells per mouse), and tumor growth was closely observed and measured every 3 days. When the tumors reached approximately 50 mm3, the mice were randomly divided into two groups (eight mice per group) and i.p. injected with the vehicle (0.8% DMSO/12% Cremophor/8% ethanol in normal saline) or 5 mg/kg longdaysin in vehicle every 3 days. This longdaysin dosage was selected based on results from preliminary experiments, and was well tolerated in the mouse model. Subsequently, tumor volumes were measured with a caliper and calculated as follows: 0.523×(length)×(width)2. After treatment for 3 weeks, the mice were sacrificed and the tumor tissues were collected and weighed before being fixed in buffered formalin .

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ERK2, ERK, Extracellular signal regulated kinases, Inhibitor, Longdaysin, inhibit, Cyclin dependent kinase, CDK, CDK7, CKIα, CKIδ, Casein Kinase, CaseinKinase

Compound Identifiers

PubChem CID

49830252