ISCK03

SKU: orb1223555

Description

A specific c-Kit inhibitor that inhibits c-kit phosphorylation in vitro and SCF-induced c-kit phosphorylation in human melanoma cells; also inhibits p44/42 ERK mitogen-activated protein kinase (MAPK) phosphorylation, does not inhibit HGF-induced phosphorylation of p44/42 ERK proteins; induces the dose-dependent depigmentation of newly regrown hair, promotes the depigmentation of UV-induced hyperpigmented spots in vivo; orally acitve.

Key Properties

• CAS Number: 945526-43-2
• MW: 355.45394
• Purity: >98% (HPLC)
• Formula: C₁₉H₂₁N₃O₂S
• SMILES: O=S(N(C1=CC=C(C(C)(C)C)C=C1)C2=CC=C(N3C=CN=C3)C=C2)=O
• Target: c-Kit
• Solubility: DMSO: ≥ 38 mg/mL

Bioactivity

• In Vivo:
  Oral administration of ISCK03 induces the dose-dependent depigmentation of newly regrown hair, and this is reversed with cessation of ISCK03 treatment. The topical application of ISCK03 promotes the depigmentation of UV-induced hyperpigmented spots. Fontana-Masson staining analysis shows epidermal melanin is diminished in spots treated with ISCK03.
• In Vitro:
  Pretreatment of 501mel cells with ISCK03 inhibits SCF-induced c-kit phosphorylation dose dependently. ISCK03 also inhibits p44/42 ERK mitogen-activated protein kinase (MAPK) phosphorylation, which is known to be involved in SCF/c-kit downstream signaling. However ISCK03 does not inhibit hepatocyte growth factor (HGF)-induced phosphorylation of p44/42 ERK proteins. ISCK03, a tyrosine kinase inhibitor specific to KIT, prevents survival of CCDC26-KD cells under low-serum conditions. All treated cells exhibits sensitivity to ISCK03 in a dose-dependent manner. After ISCK03 treatment, the survival of KD cells is suppressed to the same level as that of non-KD cells. Conversely, ISCK03 treatment has limited effects on the growth of control K562 and KD clone 3-4 cells under high-serum concentration conditions.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ISCK 03 | ISCK-03

Quick Database Links

Gene Symbol

c-Kit