iKIX1|cas:656222-54-7|西域试剂

iKIX1,99.36%

产品编号：Bellancom-124952| CAS NO：656222-54-7| 分子式：C₁₀H₈Cl₂N₄OS| 分子量：303.17

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-124952	￥800.00	杭州北京（现货）
Bellancom-124952	￥1500.00	杭州北京（现货）
Bellancom-124952	￥3000.00	杭州北京（现货）
Bellancom-124952	￥4500.00	杭州北京（现货）
Bellancom-124952	￥6500.00	杭州北京（现货）

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iKIX1

产品介绍

iKIX1 是一种抗真菌剂 (antifungal agent)，可在体外使耐药的光滑毛囊念珠菌对唑类抗真菌剂重新敏感。iKIX1 抑制介体亚基 CgGal11A 的 KIX 结构域与 CgPdr1 的激活结构域之间的相互作用，IC₅₀ 和 K_i分别为 190.2 μM 和 18 μM。iKIX1 用于研究多药耐药性和光滑念珠菌感染。

生物活性

iKIX1 is an antifungal agent and resensitizes drug-resistant C. glabrata to azole antifungals in vitro. iKIX1 inhibits the interaction between the KIX domain of the mediator subunit CgGal11A and the activation domain of CgPdr1, the IC₅₀ and K_i values are 190.2 μM and 18 μM, respectively. iKIX1 is used for the study of multidrug resistance and C. glabrata infection.

体外研究

iKIX1 (10-20 μg/ml) inhibits cell growth in a concentration-dependent manner in the presence of 5 µM ketoconazole (KET) in HepG2 cells.
FP titration curve showing the interaction of CgGal11A KIX domain with CgPdr1 AD30 fitted to a K_d of 319.7 nM. iKIX1 competes out CgPdr1 AD30 with an IC₅₀ of 190.2 µM . In vitro binding studies, iKIX1 reveals that the K_d of the CgPdr1 activation domain (AD) for the CgGal11A KIX domain is 0.32 µM and the apparent K_i for iKIX1 is 18 µM.
iKIX1 (0-50 µM) inhibits Ketoconazole (KET)-induced upregulation of luciferase activity in a dose-responsive manner in a Sc pdr1Δpdr3Δ strain containing plasmid-borne CgPDR1 and 3XPDRE-luciferase.
A chromatin immunoprecipitation (ChIP) assay is used to examine Gal11/Med15 recruitment to Pdr1-regulated target genes in S. cerevisiae. Ketoconazole induces Gal11/Med15 rapidly recruited to the promoters of the Pdr1 target genes PDR5 and SNQ2. iKIX1 abrogates Ketoconazole-induced recruitment of Gal11/Med15 and strongly inhibits azole-induced transcription of ScPdr1 target genes.
iKIX1 (20 μM) has an effect on the transcription of C. glabrata Pdr1-regulated genes involved in drug efflux and MDR (CgCDR1, CgCDR2 and CgYOR1). iKIX1 alone does not significantly affect Pdr1-target gene induction. But pre-treatment with iKIX1 reduces ketoconazole-induced CgPdr1 up-regulation in a durable and concentration-dependent manner.
In RNA sequencing (RNA-Seq) assay of a C. glabrata SFY114 (PDR1 wild-type) strain. Azole up-regulates Pdr1-dependent genes in both yeasts, such as the drug efflux pumps ScPDR5 and CgCDR1i. KIX1 combines azole strongly blunts expression of many azole-activated and Pdr1-dependent genes in both S.cerevisiae and C. glabrata, but iKIX1 alone affects very different sets of genes in S.cerevisiae and C. glabrata. And then iKIX1 does not significantly alter the expression of PDR1 or GAL11/MED15 affects very different sets of genes in S.cerevisiae and C. glabrata. iKIX1 (0-150 µM) restores the efficacy of azoles towards CgPDR1 gain-of-function mutants. It restores azole-sensitivity to PDR1 gain-of-function mutant strains in a concentration-dependent manner.

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

体内研究

性状

Solid

溶解性数据

In Vitro:

DMSO : 83.33 mg/mL (274.86 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.2985 mL	16.4924 mL	32.9848 mL
5 mM	0.6597 mL	3.2985 mL	6.5970 mL
10 mM	0.3298 mL	1.6492 mL	3.2985 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: 2.08 mg/mL (6.86 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (6.86 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (6.86 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.86 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (6.86 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.86 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。