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Cat. No.: HY-120429

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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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CAS No.: 1255099-06-9
Formule: C₁₈H₁₆ClN₃O₂S₂
Masse moléculaire:405.92

Stockage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (269 KB)

SKLB-163 Chemical Structure

CAS No.: 1255099-06-9

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Activité biologique
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	IC₅₀	1.8 μM Compound: 6t	Cytotoxicity against human A375 cells after 48 hrs by MTT assay Cytotoxicity against human A375 cells after 48 hrs by MTT assay	[PMID: 21262571]
A-375	IC₅₀	1.82 μM Compound: 41b; SKLB-163	Cytotoxicity against human A-375 cells assessed as inhibition of cell growth Cytotoxicity against human A-375 cells assessed as inhibition of cell growth	[PMID: 32898763]
A-431	IC₅₀	4.4 μM Compound: 6t	Cytotoxicity against human A431 cells after 48 hrs by MTT assay Cytotoxicity against human A431 cells after 48 hrs by MTT assay	[PMID: 21262571]
A549	IC₅₀	4 μM Compound: 6t	Cytotoxicity against human A549 cells after 48 hrs by MTT assay Cytotoxicity against human A549 cells after 48 hrs by MTT assay	[PMID: 21262571]
BXPC-3	IC₅₀	6.6 μM Compound: 6t	Cytotoxicity against human BxPC3 cells after 48 hrs by MTT assay Cytotoxicity against human BxPC3 cells after 48 hrs by MTT assay	[PMID: 21262571]
HCT-116	IC₅₀	1.3 μM Compound: 6t	Cytotoxicity against human HCT116 cells after 48 hrs by MTT assay Cytotoxicity against human HCT116 cells after 48 hrs by MTT assay	[PMID: 21262571]
HeLa	IC₅₀	4.9 μM Compound: 6t	Cytotoxicity against human HeLa cells after 48 hrs by MTT assay Cytotoxicity against human HeLa cells after 48 hrs by MTT assay	[PMID: 21262571]
HeLa	IC₅₀	5.13 μM Compound: 41b; SKLB-163	Antiproliferative activity against human HeLa cells assessed as cell growth inhibition Antiproliferative activity against human HeLa cells assessed as cell growth inhibition	[PMID: 32898763]
HepG2	IC₅₀	1.1 μM Compound: 6t	Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay	[PMID: 21262571]
HepG2	IC₅₀	1.1 μM Compound: 41b; SKLB-163	Cytotoxicity against human HepG2 cells assessed as inhibition of cell growth Cytotoxicity against human HepG2 cells assessed as inhibition of cell growth	[PMID: 32898763]
MCF7	IC₅₀	4.2 μM Compound: 6t	Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay	[PMID: 21262571]
MCF7	IC₅₀	4.2 μM Compound: 41b; SKLB-163	Cytotoxicity against human MCF7 cells assessed as inhibition of cell growth Cytotoxicity against human MCF7 cells assessed as inhibition of cell growth	[PMID: 32898763]
MDA-MB-468	IC₅₀	4.1 μM Compound: 6t	Cytotoxicity against human MDA-MB-468 cells after 48 hrs by MTT assay Cytotoxicity against human MDA-MB-468 cells after 48 hrs by MTT assay	[PMID: 21262571]
PC-3	IC₅₀	6.1 μM Compound: 6t	Cytotoxicity against human PC3 cells after 48 hrs by MTT assay Cytotoxicity against human PC3 cells after 48 hrs by MTT assay	[PMID: 21262571]
PC-3	IC₅₀	6.58 μM Compound: 41b; SKLB-163	Cytotoxicity against human PC-3 cells assessed as inhibition of cell growth Cytotoxicity against human PC-3 cells assessed as inhibition of cell growth	[PMID: 32898763]
SK-BR-3	IC₅₀	8.8 μM Compound: 6t	Cytotoxicity against human SK-BR-3 cells after 48 hrs by MTT assay Cytotoxicity against human SK-BR-3 cells after 48 hrs by MTT assay	[PMID: 21262571]
SK-OV-3	IC₅₀	4.8 μM Compound: 6t	Cytotoxicity against human SKOV3 cells after 48 hrs by MTT assay Cytotoxicity against human SKOV3 cells after 48 hrs by MTT assay	[PMID: 21262571]
SW480	IC₅₀	5.2 μM Compound: 6t	Cytotoxicity against human SW480 cells after 48 hrs by MTT assay Cytotoxicity against human SW480 cells after 48 hrs by MTT assay	[PMID: 21262571]
SW-620	IC₅₀	1.2 μM Compound: 6t	Cytotoxicity against human SW620 cells after 48 hrs by MTT assay Cytotoxicity against human SW620 cells after 48 hrs by MTT assay	[PMID: 21262571]
SW-620	IC₅₀	5.12 μM Compound: 41b; SKLB-163	Cytotoxicity against human SW620 cells assessed as inhibition of cell growth Cytotoxicity against human SW620 cells assessed as inhibition of cell growth	[PMID: 32898763]

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.

Chemical Information

CAS No. 1255099-06-9
Masse moléculaire 405.92
Formule C₁₈H₁₆ClN₃O₂S₂
SMILES

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

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (269 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. He J, et al. Antitumor and radiosensitizing effects of SKLB-163, a novel benzothiazole-2-thiol derivative, on nasopharyngeal carcinoma by affecting the RhoGDI/JNK-1 signaling pathway. Radiother Oncol. 2018 Oct;129(1):30-37. [Content Brief]

[2]. Peng X,et al. SKLB-163, a new benzothiazole-2-thiol derivative, exhibits potent anticancer activity by affecting RhoGDI/JNK-1 signaling pathway. Cell Death Dis. 2014 Mar 27;5(3):e1143. [Content Brief]

Calculators

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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