1. Protein Tyrosine Kinase/RTK
  2. c-Kit

ISCK03 

Cat. No.: HY-101443 Purity: 98.82%
Handling Instructions

ISCK03 is a specific SCF/c-Kit inhibitor.

For research use only. We do not sell to patients.
ISCK03 Chemical Structure

ISCK03 Chemical Structure

CAS No. : 945526-43-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 92 In-stock
5 mg USD 84 In-stock
10 mg USD 144 In-stock
25 mg USD 300 In-stock
50 mg USD 540 In-stock
100 mg USD 972 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

ISCK03 is a specific SCF/c-Kit inhibitor.

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[1]. 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[2].

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[1].

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 2.8133 mL 14.0667 mL 28.1334 mL
5 mM 0.5627 mL 2.8133 mL 5.6267 mL
10 mM 0.2813 mL 1.4067 mL 2.8133 mL
Please refer to the solubility information to select the appropriate solvent.
Kinase Assay
[1]

ATP is dispensed into 384-well plates, chemical compounds (ISCK03: 2.5, 5, 10, 100 μM) are added by replicative plate, and recombinant human c-kit protein is added for the kinase reaction. Following a 45-min incubation at 37°C, the development reaction is carried out for 40 min at room temperature. After the reaction is stopped, the coumrain and fluorescein fluorescence-emission signals are detected[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

To determine any cytotoxic effects of ISCK03 on 501mel cells, MTT assays are performed with various doses of ISCK03 (1, 5, 10 μM). 501mel cells are cultured with SCF alone (50 ng/mL) or SCF with ISCK03 for 48 h[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

ISCK03 is prepared in PG:EtOH:water (5:3:2).

Mice: To induce the hair cycle, depilation of skin on the back of the female C57BL/6 mice is performed. Briefly, the hair is removed from anesthetized mice. The rat antimouse c-kit-neutralizing monoclonal antibody ACK2 is administered intraperitoneally (50 mg) every day. ISCK03 is administered orally once a day. On days 21–28, animals are sacrificed or analyzed for repigmentation of the newly regrown hair shaft. Skin is harvested and fixed in paraffin or frozen for immunohistochemical analyses[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

355.45

Formula

C₁₉H₂₁N₃O₂S

CAS No.

945526-43-2

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 38 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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ISCK03
Cat. No.:
HY-101443
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