2. Metabolic Enzyme/Protease NF-κB
  3. E1/E2/E3 Enzyme Keap1-Nrf2
  4. DI-1548

DI-1548 是一种强效、选择性、不可逆的 DCN1 共价抑制剂 (IC50 = 4.6 nM)。DI-1548 能在纳摩尔浓度下强效且选择性地抑制 Cullin 3 的 neddylation 修饰，对其它 Cullin 蛋白 (包括 Cullin 1、 2、 4A、 4B 和 5) 的 neddylation 过程无明显影响，且无细胞毒性。DI-1548 与 DCN1 的共价结合会破坏 DCN1-UBC12 相互作用，导致 neddylation 复合物崩解，进而使 CRL3 失活，最终导致 NRF2 积累及其靶基因的上调，从而在小鼠模型中起到保护肝脏的作用。DI-1548 可用于肝损伤相关研究。

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DI-1548

DI-1548 Chemical Structure

CAS No. : 2247060-97-3

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DI-1548 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

DI-1548 is a potent, selective, and irreversible covalent inhibitor of DCN1 (IC50 = 4.6 nM). DI-1548 potently and selectively inhibits cullin 3 neddylation at nanomolar concentrations, and exhibits no obvious effect on the neddylation of other cullin members (including cullin 1, 2, 4A, 4B, and 5). DI-1548 exhibits no cytotoxicity. DI-1548 covalently binds to DCN1, disrupting the DCN1-UBC12 interaction, causing the collapse of the neddylation complex, inactivating CRL3, leading to NRF2 accumulation and upregulation of its target genes, and ultimately protecting mice from liver damage. DI-1548 can be used in liver injury research[1].

体外研究
(In Vitro)

DI-1548 (1-1000 nM，24 小时) 在 U2OS 细胞中，在低至 1 nM 的浓度下即可抑制 cullin 3 的 neddylation 修饰，其效力比 DI-591 (HY-124602) 强约 1000 倍[1]。
DI-1548 (0.3-1000 nM，24 小时) 在多种细胞系 (包括 U2OS、 MDA-MB-231、 KYSE70 和 HCT116) 中，能抑制 Cullin 3 的 neddylation 修饰，且对其他 Cullin 蛋白成员的选择性超过 1000 倍[1]。
DI-1548 (0-1000 nM，72 小时) 在浓度高达 1000 nM 时，对 U2OS、 MDA-MB-231、 HCT116 和 KYSE70 细胞均无细胞毒性[1]。
DI-1548 (30 nM，0-48 小时) 能快速且持久地选择性抑制 Cullin 3 (而非 Cullin 1) 的 neddylation 修饰[1]。
DI-1548 (0.3-1000 nM，1 小时) 在纳摩尔浓度下以剂量依赖性方式选择性地强效稳定细胞内的 DCN1 蛋白，对 DCN3 无明显影响[1]。

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

DI-1548 相关抗体:

Western Blot Analysis[1]

Cell Line: U2OS cells
Concentration: 1, 10, 100 and 1000 nM
Incubation Time: 24 h
Result: Reduced N-Cul3 levels at 1 nM and was approximately 1000 times more potent than DI-591.

Western Blot Analysis[1]

Cell Line: U2OS, MDA-MB-231, HCT116 and KYSE70 cells
Concentration: 0.3, 1, 3, 10, 30, 100, and 1000 nM
Incubation Time: 24 h
Result: Significantly reduced the level of N-CUL3 at concentrations as low as 0.3 nM, and achieved profound inhibition of the neddylation of cullin 3 at 1-3 nM.
Demonstrate over 300-fold greater potency than DI-591 across various cell lines.
Had no obvious effect on the neddylation of other cullin members that were examined, including cullin 1, 2, 4A, 4B, and 5 at concentrations up to 1000 nM.
Induced significant accumulation of NRF2 protein at concentrations as low as 0.3-1 nM, and was 100-1000 times more potent than DI-591.
Had no obvious effect on protein levels of KEAP1 and p62 in U2OS cells.
Had no effect on the levels of p21 and BIM proteins, substrates of CRL1, and CDT1, a substrate of CRL4A, at concentrations up to 1000 nM, consistent with its inability to inhibit neddylation of these cullin members.

Cell Viability Assay[1]

Cell Line: U2OS, MDA-MB-231, HCT116 and KYSE70 cells
Concentration: 0-1000 nM
Incubation Time: 72 h
Result: Showed no cytotoxicity in four cancer cell lines at concentrations up to 1000 nM.

Western Blot Analysis[1]

Cell Line: U2OS cells
Concentration: 30 nM
Incubation Time: 5 and 30 min,6, 24, and 48 h
Result: Inhibited the neddylation of cullin 3 within 5min but had no effect on the neddylation of cullin 1 with treatment time up to 48 h.

Western Blot Analysis[1]

Cell Line: U2OS cells
Concentration: 0.3, 1, 3, 10, 30, 100, and 1000 nM
Incubation Time: 1 h
Result: Enhanced the thermal stability of DCN1 protein in a dose-dependent manner at concentrations as low as 0.3 nM.
Exhibited over 1000-fold greater potency than DI-591 in enhancing the thermal stability of cellular DCN1 protein.
Showed no discernible effect on the thermal stability of cellular DCN3 protein at concentrations up to 1000 nM.
体内研究
(In Vivo)

DI-1548 (25 mg/kg，腹腔注射，单次给药) 可升高 C57BL/6 野生型小鼠肝脏中的 NRF2 蛋白水平[1]。

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

Animal Model: Male C57BL/6 WT mice (~8 weeks) [1]
Dosage: 25 mg/kg
Administration: i.p., once
Result: Induced robust upregulation of NRF2 protein in the mouse liver.
Produced a sustained PD effect in the liver despite being cleared from systemic circulation within 3 hours.
分子量

597.81

Formula

C32H47N5O4S
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

DI-1548 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:

DI-15482247060-97-3DI1548DI 1548E1/E2/E3 EnzymeKeap1-Nrf2E1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseDCN1cullin 3 neddylationNRF2liver injuryU2OSMDA-MB-231HCT116KYSE70Inhibitorinhibitorinhibit

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