2285446-67-3
Chemical Structure
(E/Z)-E64FC26
- CAS 番号: 2285446-67-3
- Formula:C19H23F3O2
- Molecular Weight:340.38
IUPAC Name: (E)-1-nonylidene-3-(trifluoromethyl)-1H-indene-5,6-diol
InChIKey: OWYMWLCFHDHVAH-UKTHLTGXSA-N
SMILES: OC1=CC2=C(/C(C=C2C(F)(F)F)=C/CCCCCCCC)C=C1O
Biological Activity: (E/Z)-E64FC26 is a mixture of the stereoisomers E-E64FC26 and Z-E64FC26, in which E-E64FC26 is the active component and acts as a potent PDI inhibitor. The IC50 values of E64FC26 (E-E64FC26) for PDIA1, PDIA3, PDIA4, TXNDC5, and PDIA6 are 0.6, 4.8, 33.1, 12.1, and 5.7 μM, respectively. By inhibiting PDI, (E/Z)-E64FC26 causes massive intracellular accumulation of misfolded polyubiquitinated proteins, thereby triggering strong endoplasmic reticulum stress and oxidative stress responses, which in turn induce apoptosis. (E/Z)-E64FC26 is used in research on multiple myeloma, ovarian cancer, and breast cancer[1][2][3][4].
| 製品番号 | 製品名 | 純度 | 製品説明 | Pricing | |||||||||||||||||||
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(E/Z)-E64FC26 | 99.80% | (E/Z)-E64FC26 is a mixture of the stereoisomers E-E64FC26 and Z-E64FC26, in which E-E64FC26 is the active component and acts as a potent PDI inhibitor. The IC50 values of E64FC26 (E-E64FC26) for PDIA1, PDIA3, PDIA4, TXNDC5, and PDIA6 are 0.6, 4.8, 33.1, 12.1, and 5.7 μM, respectively. By inhibiting PDI, (E/Z)-E64FC26 causes massive intracellular accumulation of misfolded polyubiquitinated proteins, thereby triggering strong endoplasmic reticulum stress and oxidative stress responses, which in turn induce apoptosis. (E/Z)-E64FC26 is used in research on multiple myeloma, ovarian cancer, and breast cancer. | ||||||||||||||||||||
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References
- [1]. Robinson RM, et al. Tuning isoform selectivity and bortezomib sensitivity with a new class of alkenyl indene PDI inhibitor. European journal of medicinal chemistry. 2020 Jan 15;186:111906.
- [2]. Liu W, et al. Rational identification of a Cdc42 inhibitor presents a new regimen for long-term hematopoietic stem cell mobilization. Leukemia. 2019 Mar;33(3):749-761.
- [3]. Xu S, et al. Discovery of an orally active small-molecule irreversible inhibitor of protein disulfide isomerase for ovarian cancer treatment. Proceedings of the National Academy of Sciences of the United States of America. 2012 Oct 02;109(40):16348-53. [Content Brief]
- [4]. Daurio NA, et al. AMPK Activation and Metabolic Reprogramming by Tamoxifen through Estrogen Receptor-Independent Mechanisms Suggests New Uses for This Therapeutic Modality in Cancer Treatment. Cancer research. 2016 Jun 01;76(11):3295-306.
