2. PROTAC Metabolic Enzyme/Protease
  3. PROTACs Indoleamine 2,3-Dioxygenase (IDO)
  4. NU223612

NU223612 是一种有效的 PROTAC (PROTACs)，可降解吲哚胺 2,3-双加氧酶 1 (IDO1) (Indoleamine 2,3-Dioxygenase (IDO))，Kd 为 640 nM。NU223612 通过 CRBN 介导的蛋白酶体降解有效降解 IDO1 蛋白。NU223612 以 290 nM 的亲和力与 CRBN 结合。NU223612 可以穿过血脑屏障 (BBB)。

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NU223612 Chemical Structure

NU223612 Chemical Structure

CAS No. : 2759420-43-2

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NU223612 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

查看所有亚型
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

查看 Indoleamine 2,3-Dioxygenase (IDO) 亚型特异性产品:

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IDO1 IDO2 IDO

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

NU223612 is a potent PROTAC (PROTACs) that degrades indoleamine 2,3-dioxygenase 1 (IDO1) (Indoleamine 2,3-Dioxygenase (IDO)) with a Kd of 640 nM. NU223612 potently degrades the IDO1 protein through CRBN-mediated proteasomal degradation. NU223612 is bound to CRBN with an affinity of 290 nM. NU223612 can cross the blood-brain barrier (BBB)[1].

IC50 & Target[1]

Cereblon

 

IDO1

640 nM (Kd)

体外研究
(In Vitro)

NU223612 (0.1-10 μM; 24 h) decreases IDO1 protein levels dose-dependently[1].
A DC50 (the concentration of the NU223612 at which 50% of the IDO1 protein is degraded) of 0.3290 μM and 0.5438 μM in U87 and GBM43 cells is determined, respectively[1].
NU223612 degrades IDO1 protein in multiple cell types, such as CD18 and PANC-1 human pancreatic cancer cells, OVCAR5 and SKOV3 human ovarian cancer cells, PC3 human prostate cancer cells, and the syngeneic GL261 mouse IDO1 cDNA-expressing (IDO1-O/E) glioma cell line[1].
NU223612 equally degrades IDO1 protein levels in both the cytoplasmic and nuclear intracellular compartments in human GBM cells. NU223612 is able to penetrate subcellular compartments[1].
NU223612 dose-dependently inhibits IDO1 enzyme activity resulting in decreased Kyn levels in cultured IFNγ-stimulated GBM cells. NU223612 inhibits both IDO1-mediated tryptophan metabolism as well as IDO1 non-enzyme-mediated NF-κB p65 transcription factor DNA binding activity[1].

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

NU223612 相关抗体:

Western Blot Analysis[1]

Cell Line: U87 and human GBM43 cells
Concentration: 0 μM, 0.1 μM, 1 μM, and 10 μM
Incubation Time: 24 h
Result: Decreased IDO1 protein levels dose-dependently.
体内研究
(In Vivo)

NU223612 (25 mg/kg; i.p.; once) decreases IDO1 protein in C57BL/6 with mIDO1 cDNA-expressing GL261 cells[1].
NU223612 (25 mg/kg; i.p.; 5 days/week; for 3 weeks) leads to an increase in median overall survival as well as longer-term survival for up to 45 days post-tumor cell injection[1].
Mass spectrometry analysis of NU223612 (25 mg/kg; i.p.; once) shows a Cmax of 2 μM and a half-life of 8.3 h in brain tissue. In plasma, Cmax is 365 μM and the half-life is 2.5 h. The binding of NU223612 to mouse brain homogenate using a 6 h equilibrium dialysis shows NU223612 to be 99.8% bound[1].
Half-life, AUC, and?Cmax?of?NU223612?in serum and brain samples[1].

Plasma Brain
half-lifr (h) 2.5 8.3
AUC0-24 (μM?h) 582 7
Cmax (μM) 365 2

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

Animal Model: Male C57BL/6 mice bearing GL261 cells[1]
Dosage: 25 mg/kg
Administration: i.p.; once
Result: Decreased IDO1 protein by >70% within 2 h post-treatment and remains low for up to 24 h.
Animal Model: 8 week old C57BL/6 wild-type (WT) mice are intracranially engrafted with luciferase-modified GL261 cells (GL261-luc.)[1]
Dosage: 25 mg/kg
Administration: i.p.; 5 days/week; for 3 weeks
Result: Led to an increase in median overall survival as well as longer-term survival for up to 45 days post-tumor cell injection.
分子量

890.99

Formula

C49H55FN6O9
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

NU223612 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:

NU2236122759420-43-2NU 223612NU-223612PROTACsIndoleamine 2,3-Dioxygenase (IDO)glioblastomaIDO1-PROTACCRBNproteasomal degradationblood-brain barrierNF-κB phosphorylationInhibitorinhibitorinhibit

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