2. Immunology/Inflammation
  3. IKZF Family IFNAR
  4. NHWL071065

NHWL071065 是一种 IKZF1/IKZF3 降解剂。NHWL071065 可通过泛素-蛋白酶体途径选择性降解淋巴瘤细胞中的 IKZF1 和 IKZF3。NHWL071065 可抑制淋巴瘤细胞的增殖。NHWL071065 下调细胞中参与细胞骨架组装、细胞黏附和免疫调控的蛋白，同时上调 I 型 IFN 信号通路相关蛋白。NHWL071065 可用于淋巴瘤的研究。

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NHWL071065

NHWL071065 Chemical Structure

CAS No. : 3117340-01-6

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NHWL071065 相关抗体

Top Publications Citing Use of Products

查看 IKZF Family 亚型特异性产品:

查看所有亚型
IKZF1 IKZF2 IKZF3 IKZF4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

NHWL071065 is a IKZF1/IKZF3 degrader. NHWL071065 selectively degrades IKZF1 and IKZF3 in lymphoma cells via the ubiquitin-proteasome pathway. NHWL071065 inhibits the proliferation of lymphoma cells. NHWL071065 downregulates proteins involved in cytoskeleton assembly, cell adhesion and immune regulation in cells, while upregulating proteins related to the type I IFN signaling pathway. NHWL071065 can be used in the research of lymphoma[1].

IC50 & Target[1]

IKZF1

 

IKZF3

 

体外研究
(In Vitro)

NHWL071065 (Compound 26) (3 days) 可强效抑制 TMD8 细胞 (IC50 = 6.6 nM) 和 WSU-DLCL2 细胞 (IC50 = 2.6 nM) 的增殖，但对 MKN28、PANC-1、LO2 或 HUVEC 细胞无抑制活性[1]。
NHWL071065 (1.25-40 nM, 0.313-5 μM; 16 h) 可在 TMD8 细胞中强效且选择性地降解 IKZF1 (DC50 = 1.8 nM) 和 IKZF3 (DC50 = 14.9 nM)，并在 WSU-DLCL2 细胞中呈浓度依赖性地降解 IKZF1/IKZF3，且不会降解 PDE6D、SALL4 或 GSPT1[1]。
NHWL071065 (100 nM; 6 h) 可显著下调 TMD8 细胞中的 IKZF1/IKZF3 以及参与细胞骨架组装、细胞黏附和免疫调控的蛋白，同时上调 I 型干扰素信号通路相关蛋白，但对 GSPT1、NEK7 或 CK1α 无显著影响[1]。

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

NHWL071065 相关抗体:

Western Blot Analysis[1]

Cell Line: TMD8 lymphoma cells, WSU-DLCL2 lymphoma cells
Concentration: 1.25, 2.5, 5, 10, 20, 40 nM (TMD8 cells, IKZF1/IKZF3); 1, 5, 10, 50 nM (WSU-DLCL2 cells, IKZF1/IKZF3); 0.313, 0.625, 1.25, 2.5, 5 μM (TMD8 cells, PDE6D/SALL4); 1, 5, 10, 50 nM (TMD8 cells, GSPT1)
Incubation Time: 16 h
Result: Achieved a DC50 of 1.8 nM for IKZF1 degradation and 14.9 nM for IKZF3 degradation in TMD8 cells, with near-complete degradation at 40 nM.
Concentration-dependently degraded both IKZF1 and IKZF3 in WSU-DLCL2 cells, with significant reduction observed at 1 nM.
Did not degrade PDE6D (up to 5 μM), SALL4 (up to 2.5 μM), or GSPT1 (at concentrations that potently degrade IKZF1/3) in TMD8 cells.
药代动力学
(Parmacokinetics)
Species Dose Route AUC0-∞ MRT0-∞ T1/2β Tmax Vz Cmax
Rat[1] 2 mg/kg i.v. 1078.319 μg/L·h 5.807 h 6.395 h / 17.456 L/kg 2330 μg/L
Rat[1] 10 mg/kg p.o. 1105.037 μg/L·h 8.046 h 5.913 h 0.667 h 77.406 L/kg 157.667 μg/L
分子量

576.66

Formula

C31H37FN6O4
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

NHWL071065 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:

NHWL0710653117340-01-6NHWL 071065NHWL-071065IKZF FamilyIFNARIkaros zinc finger protein familyInterferon-α/β receptorInterferon-alpha/beta receptorIKZF1TMD8 cellsCRBN E3 ligase modulatorlymphomaWSU-DLCL2 cellsIKZF3type I interferon signaling pathwayhuman liver microsomesubiquitin-proteasome pathwaylymphoma cellsInhibitorinhibitorinhibit

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NHWL071065
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