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ISCK03 is an inhibitor of SCF-mediated c-kit activation.

The signaling downstream of SCF/c-kit plays a key role in the development of various mammalian cells, such as mast cells, melanocytes, primordial germ cells, and hematopoietic progenitor cells.

In vitro: Previous study showed that the pretreatment of 501mel cells with ISCK03 could dose-dependently inhibit SCF-induced c-kit phosphorylation. ISCK03 could also inhibit the phosphorylation of p44/42 ERK mitogen-activated protein kinase that was known to be involved in SCF/c-kit downstream signaling. However, ISCK03 was not able to inhibit hepatocyte growth factor-induced phosphorylation of p44/42 ERK proteins [1].

In vivo: To determine the in vivo efficacy, ISCK03was orally administered to depilated C57BL/6 mice. Results showed that the oral administration of ISCK03 could induce the dose-dependent depigmentation of newly regrown hair, and this was reversed with cessation of ISCK03 treatment. In addition, the topical application of ISCK03 could promote the depigmentation of UV-induced hyperpigmented spots on n brownish guinea pig skin. Moreover, the Fontana–Masson staining analyses showed epidermal melanin was diminished in spots treated with ISCK03 [1].

Clinical trial: Up to now, ISCK03 is still in the preclinical development stage.

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