WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H466000
CAS#: unknown
Description: USP30i is a novel USP30 inhibitor, increasing Ub-TOM20 with an EC50 of 2.45 mM and inducing the maximal Ub-TOM20.
Hodoodo Cat#: H466000
Name: USP30i
CAS#: unknown
Chemical Formula: C15H16N4S
Exact Mass: 284.11
Molecular Weight: 284.381
Elemental Analysis: C, 63.35; H, 5.67; N, 19.70; S, 11.27
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Synonym: USP30i; USP 30i; USP-30i;
IUPAC/Chemical Name: (R)-3-(((5-phenylthiazol-2-yl)amino)methyl)pyrrolidine-1-carbonitrile
InChi Key: XRKWRSYZFZXPNK-GFCCVEGCSA-N
InChi Code: InChI=1S/C15H16N4S/c16-11-19-7-6-12(10-19)8-17-15-18-9-14(20-15)13-4-2-1-3-5-13/h1-5,9,12H,6-8,10H2,(H,17,18)/t12-/m1/s1
SMILES Code: N#CN1C[C@@H](CNC2=NC=C(C3=CC=CC=C3)S2)CC1
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: To be determined
Shelf Life: >2 years if stored properly
Drug Formulation: To be determined
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
Biological target: | |
In vitro activity: | |
In vivo activity: |
The following data is based on the product molecular weight 284.38 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
Formulation protocol: | |
In vitro protocol: | |
In vivo protocol: |
1: Zhang R, Ozgen S, Luo H, Krigman J, Zhao Y, Xin G, Sun N. The Mitochondrial Deubiquitinase USP30 Regulates AKT/mTOR Signaling. Front Pharmacol. 2022 Feb 17;13:816551. doi: 10.3389/fphar.2022.816551. PMID: 35250566; PMCID: PMC8891576.
2: Qin X, Wang R, Xu H, Tu L, Chen H, Li H, Liu N, Wang J, Li S, Yin F, Xu N, Li Z. Identification of an autoinhibitory, mitophagy-inducing peptide derived from the transmembrane domain of USP30. Autophagy. 2022 Jan 6:1-20. doi: 10.1080/15548627.2021.2022360. Epub ahead of print. PMID: 34989313.
3: Li X, Wang T, Tao Y, Wang X, Li L, Liu J. MF-094, a potent and selective USP30 inhibitor, accelerates diabetic wound healing by inhibiting the NLRP3 inflammasome. Exp Cell Res. 2022 Jan 15;410(2):112967. doi: 10.1016/j.yexcr.2021.112967. Epub 2021 Dec 6. PMID: 34883112.
4: Rusilowicz-Jones EV, Barone FG, Lopes FM, Stephen E, Mortiboys H, Urbé S, Clague MJ. Benchmarking a highly selective USP30 inhibitor for enhancement of mitophagy and pexophagy. Life Sci Alliance. 2021 Nov 29;5(2):e202101287. doi: 10.26508/lsa.202101287. PMID: 34844982; PMCID: PMC8645336.
5: Cabrera SF, Muratore ME, Buijnsters P. The intriguing role of USP30 inhibitors as deubiquitinating enzymes from the patent literature since 2013. Expert Opin Ther Pat. 2021 Nov 8. doi: 10.1080/13543776.2022.2003780. Epub ahead of print. PMID: 34743664.
6: Tsefou E, Walker AS, Clark EH, Hicks AR, Luft C, Takeda K, Watanabe T, Ramazio B, Staddon JM, Briston T, Ketteler R. Investigation of USP30 inhibition to enhance Parkin-mediated mitophagy: tools and approaches. Biochem J. 2021 Dec 10;478(23):4099-4118. doi: 10.1042/BCJ20210508. PMID: 34704599; PMCID: PMC8718267.
7: Wang N, Li J, Xin Q, Xu N. USP30-AS1 contributes to mitochondrial quality control in glioblastoma cells. Biochem Biophys Res Commun. 2021 Dec 3;581:31-37. doi: 10.1016/j.bbrc.2021.10.006. Epub 2021 Oct 9. PMID: 34653676.
8: Luo H, Krigman J, Zhang R, Yang M, Sun N. Pharmacological inhibition of USP30 activates tissue-specific mitophagy. Acta Physiol (Oxf). 2021 Jul;232(3):e13666. doi: 10.1111/apha.13666. Epub 2021 Apr 29. PMID: 33890401; PMCID: PMC8266733.
9: Gu L, Zhu Y, Lin X, Lu B, Zhou X, Zhou F, Zhao Q, Prochownik EV, Li Y. The IKKβ-USP30-ACLY Axis Controls Lipogenesis and Tumorigenesis. Hepatology. 2021 Jan;73(1):160-174. doi: 10.1002/hep.31249. Epub 2020 Nov 6. PMID: 32221968.
10: Miller S, Muqit MMK. Therapeutic approaches to enhance PINK1/Parkin mediated mitophagy for the treatment of Parkinson's disease. Neurosci Lett. 2019 Jul 13;705:7-13. doi: 10.1016/j.neulet.2019.04.029. Epub 2019 Apr 14. PMID: 30995519.
11: Kluge AF, Lagu BR, Maiti P, Jaleel M, Webb M, Malhotra J, Mallat A, Srinivas PA, Thompson JE. Novel highly selective inhibitors of ubiquitin specific protease 30 (USP30) accelerate mitophagy. Bioorg Med Chem Lett. 2018 Aug 15;28(15):2655-2659. doi: 10.1016/j.bmcl.2018.05.013. Epub 2018 May 8. PMID: 29935771.
12: Liang JR, Martinez A, Lane JD, Mayor U, Clague MJ, Urbé S. USP30 deubiquitylates mitochondrial Parkin substrates and restricts apoptotic cell death. EMBO Rep. 2015 May;16(5):618-27. doi: 10.15252/embr.201439820. Epub 2015 Mar 4. PMID: 25739811; PMCID: PMC4428036.
13: Escobar-Henriques M. Mitofusins: ubiquitylation promotes fusion. Cell Res. 2014 Apr;24(4):387-8. doi: 10.1038/cr.2014.23. Epub 2014 Feb 21. PMID: 24556809; PMCID: PMC3975502.
14: Yue W, Chen Z, Liu H, Yan C, Chen M, Feng D, Yan C, Wu H, Du L, Wang Y, Liu J, Huang X, Xia L, Liu L, Wang X, Jin H, Wang J, Song Z, Hao X, Chen Q. A small natural molecule promotes mitochondrial fusion through inhibition of the deubiquitinase USP30. Cell Res. 2014 Apr;24(4):482-96. doi: 10.1038/cr.2014.20. Epub 2014 Feb 11. PMID: 24513856; PMCID: PMC3975501.
15: Buus R, Faronato M, Hammond DE, Urbé S, Clague MJ. Deubiquitinase activities required for hepatocyte growth factor-induced scattering of epithelial cells. Curr Biol. 2009 Sep 15;19(17):1463-6. doi: 10.1016/j.cub.2009.07.040. Epub 2009 Aug 20. PMID: 19699092; PMCID: PMC2764384.