2. Metabolic Enzyme/Protease Immunology/Inflammation GPCR/G Protein Apoptosis
  3. Ser/Thr Kinase CXCR TNF Receptor Interleukin Related
  4. DF-003

DF-003 是一种具有选择性、口服活性、ATP 竞争性且可透过血脑屏障的 ALPK1 抑制剂。DF-003 强效抑制人类 ALPK1 和 ALPK1[T237M]，IC50s 值分别为 1.5 nM 和 16 nM。DF-003 的选择性比最接近的激酶高出 860 倍以上。DF-003 可抑制 HEK-293 细胞中 TNF、CXCL10 或 CXCL8 的上调。DF-003 可用于视网膜营养不良、视神经水肿、脾肿大、无汗症和头痛 (ROSAH) 综合征的研究。

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DF-003

DF-003 Chemical Structure

CAS No. : 2765462-07-3

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DF-003 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

DF-003 is a selective, orally active, ATP-competitive, and brain-penetrant ALPK1 inhibitor. DF-003 potently inhibits human ALPK1 and ALPK1[T237M] with IC50s value of 1.5 nM and 16 nM. DF-003 exhibits more than 860-fold selectivity over the closest kinase. DF-003 inhibits TNF, CXCL10, or CXCL8 upregulation in HEK-293 cells. DF-003 can be used for the study of retinal dystrophy, optic nerve edema, splenomegaly, anhidrosis, and headache (ROSAH) syndrome[1].

IC50 & Target

IL-6

 

体外研究
(In Vitro)

DF-003 (1-50.8 pM，60 小时) 剂量依赖性地抑制 ALPK1 激酶活性 (IC50 = 1.5 nM)[1]。
DF-003 (20 μM-0.763 nM，2 小时) 对 TAOK2/TAO1 (IC50=1.29 µM)、CAMK2g (IC50 = 3.10 µM) 和 CAMK1a (IC50 = 4.60 µM) 表现出非 ALPK1 激酶抑制活性[1]。
DF-003 (10-1000 nM，1 小时) 有效抑制 HEK-293 细胞中 DF-006 诱导的 TIFAsome 形成，表明其在细胞内抑制 ALPK1[1]。
DF-003 (0.3-1000 nM，2 小时) 可抑制 THP-1 细胞中 DF-006 (HY-176507) 诱导的 TNF (IC50 = 8 nM) 和 CXCL8 (IC50 = 6.5 nM) 的上调[1]。
DF-003 (1-50.8 pM，60 小时) 以剂量依赖性方式抑制 UDP-甘露糖刺激的 ALPK1[T237M] (IC50 = 16 nM)[1]。
DF-003 (0.64-20 μM，48 小时) 在缺乏外源刺激的情况下抑制 ALPK1[T237M] OE HEK293 细胞中的 NF-κB 报告基因活性[1]。
DF-003 (0.64-20 μM，30 小时) 剂量依赖性地抑制过表达 ALPK1[T237M] 的 HEK-293 细胞中细胞因子的上调，且对过表达野生型 ALPK1 的 HEK-293 细胞中 TNF、CXCL10 或 CXCL8 的基础表达无影响[1]。
DF-003 (0.64-20 μM，30 小时) 抑制过表达 ALPK1[T237M] 的 HEK-293 细胞中 CXCL8 分泌增强(IC50 = 125 nM)[1]。

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

DF-003 相关抗体:

RT-PCR[1]

Cell Line: THP-1
Concentration: 0.3-1000 nM
Incubation Time: Pretreated with 2 h, then stimulated for an additional 4 h using 5 nM DF006
Result: Exhibited the inhibition of DF-006-induced TNF (IC50 = 8 nM) and CXCL8 (IC50 = 6.5 nM) upregulation.

RT-PCR[1]

Cell Line: HEK-293 cells
Concentration: 0.64-20 μM
Incubation Time: 30 h
Result: Inhibited cytokine upregulation in HEK-293 cells overexpressing ALPK1[T237M] dose-dependently and had no impact on the basal expression of TNF, CXCL10, or CXCL8 in cells overexpressing wild-type ALPK1.

ELISA Assay[1]

Cell Line: HEK-293 cells
Concentration: 0.64-20 μM
Incubation Time: 30 h
Result: Suppressed the enhanced secretion of CXCL8 from HEK-293 cells overexpressing ALPK1[T237M] (IC50 = 125 nM).
体内研究
(In Vivo)

DF-003 (3-5 mg/kg，灌胃，每日一次，共 10 天) 能有效透过血视网膜屏障和血脑屏障，抑制ALPK1[T237M] 突变引起的多组织炎症反应，包括 hALPK1[T237M]-KI C57BL/6N 小鼠的视网膜小胶质细胞浸润、星形胶质细胞活化和炎症细胞因子表达[1]。

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

Animal Model: Female hALPK1-KI and hALPK1[T237M]-KI C57BL/6N mice[1].
Dosage: 3 mg/kg, 5 mg/kg
Administration: Oral gavage, once daily for 10 days
Result: Suppressed 68% and 53% of this microglial activation in the INL and ONL, respectively. Suppressed 49% of the increase in astrocyte activity.
Suppressed the upregulation of Ccl2, Ccl5, Cxcl1, Cxcl9, Cxcl10, Tnf, Il6, as well as the microglia marker genes Cx3cr1 and Aif1 in the retina.
Did not reveal any evidence of retinal degeneration or optic nerve/optic disc/retina edema in these ROSAH mice.
Showed no splenomegaly and anhidrosis evident in these mice at ages of up to 6 months.
分子量

486.96

Formula

C24H21ClF2N4OS
CAS 号
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.
纯度 & 产品资料
参考文献

DF-003 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • 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.

Keywords:

DF-0032765462-07-3DF003DF 003Ser/Thr KinaseCXCRTNF ReceptorInterleukin RelatedProtein Serine-Threonine KinaseCXC chemokine receptorsC-X-C motif chemokine receptorsTumor Necrosis Factor ReceptorTNFRILROSAHALPK1alpha-kinase 1T237MTNFCXCL 10CXCL 8Inhibitorinhibitorinhibit

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