1. Immunology/Inflammation
  2. SPHK
  3. SK1-​I hydrochloride

SK1-​I hydrochloride (Synonyms: BML-258 hydrochloride)

目录号: HY-119016A
产品使用指南

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

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SK1-​I hydrochloride Chemical Structure

SK1-​I hydrochloride Chemical Structure

CAS No. : 2366222-05-9

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Description

SK1-I hydrochloride (BML-258 hydrochloride), an analog of sphingosine, is an isozyme-specific competitive SPHK1 inhibitor with a Ki value of 10 µM[1]. SK1-I hydrochloride (BML-258 hydrochloride) has good water solubility. SK1-I hydrochloride (BML-258 hydrochloride) shows no activity at SPHK1 PKCα, PKCδ, PKA, AKT1, ERK1, EGFR, CDK2, IKKβ or CamK2β. SK1-I hydrochloride (BML-258 hydrochloride) enhances autophagy and has antitumor activity[2].

IC50 & Target

Ki: 10 µM (SPHK1)[1]

In Vitro

SK1-I hydrochloride (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[2].
SK1-I hydrochloride (0-20 μM; 12 hours) induces more CASP3 cleavage in HCT116 cells, compared to HCT116 cells lacking TP53, leading to a hallmark of apoptosis[2].

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

Cell Viability Assay[2]

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[2]

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.
In Vivo

Pre-treatment with SK1-I hydrochloride (BML-258 hydrochloride; 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[3].

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

Animal Model: Male C57BL/6 mice (24 ± 3.5 g) [3]
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).
Molecular Weight

313.86

Formula

C₁₇H₂₈ClNO₂

CAS No.

2366222-05-9

SMILES

OC[C@H]([C@H](/C=C/C1=CC=C(C=C1)CCCCC)O)NC.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

SK1-​IBML-258BML258BML 258SPHKSphingosine kinasecompetitiveantitumorautophagyInhibitorinhibitorinhibit

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产品名称:
SK1-​I hydrochloride
目录号:
HY-119016A
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