VLX1570

VLX1570
Identifiers
	IUPAC name (3E,5E)-3,5-bis[(4-fluoro-3-nitrophenyl)methylidene]-1-prop-2-enoylazepan-4-one;
CAS Number	1956378-23-6;
PubChem CID	71523377;
Chemical and physical data
Formula	C23H17F2N3O6
Molar mass	469.401 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES C=CC(=O)N1CC/C(=C\C2=CC(=C(C=C2)F)[N+](=O)[O-])/C(=O)/C(=C/C3=CC(=C(C=C3)F)[N+](=O)[O-])/C1;
	InChI InChI=1S/C23H17F2N3O6/c1-2-22(29)26-8-7-16(9-14-3-5-18(24)20(11-14)27(31)32)23(30)17(13-26)10-15-4-6-19(25)21(12-15)28(33)34/h2-6,9-12H,1,7-8,13H2/b16-9+,17-10+; Key:SCKXBVLYWLLALY-CZCYGEDCSA-N;

VLX1570 is a drug used in scientific research which acts as a non selective inhibitor of proteasome deubiquitinases. It has potential applications in the treatment of cancer, though was discontinued in clinical trials due to excessive toxicity.^[1]^[2]^[3]^[4]

References

^ Stanton C, Sun J, Nutsch K, Rosarda JD, Nguyen T, Li-Ma C, et al. (February 2024). "Covalent Targeting As a Common Mechanism for Inhibiting NLRP3 Inflammasome Assembly". ACS Chemical Biology. 19 (2): 254–265. doi:10.1021/acschembio.3c00330. PMC 11131128. PMID 38198472.
^ Bazzaro M, Linder S (December 2020). "Dienone Compounds: Targets and Pharmacological Responses". Journal of Medicinal Chemistry. 63 (24): 15075–15093. doi:10.1021/acs.jmedchem.0c00812. PMC 7770821. PMID 33146523.
^ Rowinsky EK, Paner A, Berdeja JG, Paba-Prada C, Venugopal P, Porkka K, et al. (October 2020). "Phase 1 study of the protein deubiquitinase inhibitor VLX1570 in patients with relapsed and/or refractory multiple myeloma". Investigational New Drugs. 38 (5): 1448–1453. doi:10.1007/s10637-020-00915-4. PMC 7497669. PMID 32125598.
^ Wang J, Du T, Lu Y, Lv Y, Du Y, Wu J, et al. (January 2022). "VLX1570 regulates the proliferation and apoptosis of human lung cancer cells through modulating ER stress and the AKT pathway". Journal of Cellular and Molecular Medicine. 26 (1): 108–122. doi:10.1111/jcmm.17053. PMC 8742231. PMID 34854221.

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[1] Stanton C, Sun J, Nutsch K, Rosarda JD, Nguyen T, Li-Ma C, et al. (February 2024). "Covalent Targeting As a Common Mechanism for Inhibiting NLRP3 Inflammasome Assembly". ACS Chemical Biology. 19 (2): 254–265. doi:10.1021/acschembio.3c00330. PMC 11131128. PMID 38198472.

[2] Bazzaro M, Linder S (December 2020). "Dienone Compounds: Targets and Pharmacological Responses". Journal of Medicinal Chemistry. 63 (24): 15075–15093. doi:10.1021/acs.jmedchem.0c00812. PMC 7770821. PMID 33146523.

[3] Rowinsky EK, Paner A, Berdeja JG, Paba-Prada C, Venugopal P, Porkka K, et al. (October 2020). "Phase 1 study of the protein deubiquitinase inhibitor VLX1570 in patients with relapsed and/or refractory multiple myeloma". Investigational New Drugs. 38 (5): 1448–1453. doi:10.1007/s10637-020-00915-4. PMC 7497669. PMID 32125598.

[4] Wang J, Du T, Lu Y, Lv Y, Du Y, Wu J, et al. (January 2022). "VLX1570 regulates the proliferation and apoptosis of human lung cancer cells through modulating ER stress and the AKT pathway". Journal of Cellular and Molecular Medicine. 26 (1): 108–122. doi:10.1111/jcmm.17053. PMC 8742231. PMID 34854221.

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