ISCK03

Research use only, not for human use.

A specific c-Kit inhibitor that inhibits c-kit phosphorylation in vitro and SCF-induced c-kit phosphorylation in human melanoma cells.

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.

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.

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.

ISCK 03 | ISCK-03

Angiogenesis

c-Kit

c-Kit

Cancer

——

945526-43-2

355.45394

C19H21N3O2S

>98% (HPLC)

DMSO: ≥ 38 mg/mL

O=S(N(C1=CC=C(C(C)(C)C)C=C1)C2=CC=C(N3C=CN=C3)C=C2)=O

Benzenesulfonamide, 4-(1,1-dimethylethyl)-N-[4-(1H-imidazol-1-yl)phenyl]-

(-20℃)

With Ice Pack

≥ 2 years