SK1-I - CAS:1072443-89-0

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SK1-I (Synonyms:BML-258)

目录号 : KM6550 CAS No. : 1072443-89-0

Data Sheet 产品使用指南

SK1-I (BML-258) 是鞘氨醇的类似物，是同功酶特异性 SPHK1 竞争抑制剂，K_i 值为 10 µM。SK1-I 对 SPHK2，PKCα，PKCδ，PKA，AKT1，ERK1，EGFR，CDK2，IKKβ 或 CamK2β 无活性。SK1-I 增强自噬并具有抗肿瘤活性。

规格	价格	是否有货	数量
5mg		In-stock
10mg		In-stock
25mg		In-stock
50mg		In-stock
100mg		In-stock

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生物活性

SK1-I (BML-258), an analog of sphingosine, is an isozyme-specific competitive SPHK1 inhibitor with a K_i value of 10 µM. SK1-I shows no activity at SPHK1 PKCα, PKCδ, PKA, AKT1, ERK1, EGFR, CDK2, IKKβ or CamK2β. SK1-I enhances autophagy and has antitumor activity.

体外研究

SK1-I (0-10 μM; 24 hours) attenuates cancer cell growth and survival in a TP53-dependent manner in HCT116 cells and HCT116 cells bearing TP53 null cancer.
SK1-I (0-20 μM; 12 hours) induces more CASP3 cleavage in HCT116 cells, compared to HCT116 cells lacking TP53, leading to a hallmark of apoptosis.

Cell Viability Assay

Cell Line:	HCT116 cells and HCT116 cells bearing TP53 null cancer
Concentration:	0 µM, 2.5 µM, 5 µM, 7.5 µM, 10 µM
Incubation Time:	24 hours
Result:	Decreased cancer cell growth and survival.

Western Blot Analysis

Cell Line:	HCT116 cells and HCT116 cells bearing TP53 null cancer
Concentration:	0 µM, 5 µM, 10 µM, 20 µM
Incubation Time:	12 hours
Result:	Induced more CASP3 cleavage in HCT116 cells, compared to HCT116 cells lacking TP53.

体内研究

Pre-treatment with SK1-I (BML-258; intraperitoneal (i.p.) injection; once; 24 hours prior to baseline mean arterial blood pressure (MAP) measurement; 75 mg/kg) before anandamide (i.v. injection; two doses; 1 and 10 mg/kg) significantly decreases the hypotensive response.

Animal Model:	Male C57BL/6 mice (24 ± 3.5 g)
Dosage:	75 mg/kg
Administration:	Intraperitoneal (i.p.) injection; once; 24 hours prior to baseline MAP measurement
Result:	Significantly lowered baseline mean arterial blood pressure (MAP).

分子式

C₁₇H₂₇NO₂^.HCl

分子量

277.40

CAS号

1072443-89-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

Data Sheet

产品使用指南

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

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

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