1. Apoptosis
  2. Apoptosis
  3. SKLB-163

SKLB-163 is an orally active inhibitor for Rho GDP-dissociation (RhoGDI). SKLB-163 inhibits highly expressed RhoGDI tumor cell proliferation and migration, and increases radiosensitivity of tumor cells. SKLB-163 induces cancer cell Apoptosis.

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SKLB-163 Chemical Structure

SKLB-163 Chemical Structure

CAS No. : 1255099-06-9

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Description

SKLB-163 is an orally active inhibitor for Rho GDP-dissociation (RhoGDI). SKLB-163 inhibits highly expressed RhoGDI tumor cell proliferation and migration, and increases radiosensitivity of tumor cells. SKLB-163 induces cancer cell Apoptosis[1][2].

In Vitro

SKLB-163 (0-20 μM, 48 h) inhibits proliferation and migration of nasopharyngeal carcinoma (NPC) cells, and sensitizes cells to irradiation[1].
SKLB-163 (0-20 μM, 48 h) shows cytotoxicity effect in A375, SPC-A1, SW620, HeLa, PC-3 cells[2].
SKLB-163 (0-2.5 μM, 48 h) induces A375 cell apoptosis and inhibits colony information[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

SKLB-163 (25-100 mg/kg, i.g., once daily for 30 days) inhibits tumor growth and ascites formation, and inhibits liver and lung metastasis in NPC lung metastatic mice model[1].
SKLB-163 (50 mg/kg, once daily. from the 6th day of SKLB-163 administration, 3 Gy radiation once per day for 3 days) sensitizes NPC tumor to irradiation in CNE-2 and C666-1 subcutaneous xenograft mice models[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: NPC lung metastatic model: transplanting NPC cells C666-1 into the livers of BALB/c nude mice[1]
Dosage: 25, 50, 100 mg/kg
Administration: intragastric administration, once daily for 30 days
Result: Reduced tumor size by 33.5% (25 mg/kg), 53.6% (50 mg/kg), 81.6% (100 mg/kg), respectively.
Ascited formation by 33.9% (25 mg/kg), 58.7% (50 mg/kg), 82.2% (100 mg/kg).
Inhibited liver or lung metastasis.
Molecular Weight

405.92

Formula

C18H16ClN3O2S2

CAS No.
SMILES

O=C(CSC1=NC2=CC=C(C=C2S1)NC(CCl)=O)NCC3=CC=CC=C3

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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SKLB-163
Cat. No.:
HY-120429
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