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VLX1570 - 99%, high purity , CAS No.1431280-51-1, Inhibitor of ubiquitin specific peptidase 14

COA

Grade & Purity:

Moligand™

≥99%

Cas Number: 1431280-51-1
Molecular Weight: 469.39
PubChem CID: 118989091
PubChem SID: 504772904

In stock

Item Number

V413963

Grouped product items
SKU	Size	Availability	Price
V413963-2mg	2mg	3	$156.90
V413963-5mg	5mg	3	$325.90
V413963-10mg	10mg	3	$513.90
V413963-25mg	25mg	2	$1,156.90
V413963-50mg	50mg	1	$1,533.90
V413963-100mg	100mg	1	$2,375.90

Competitive inhibitor of proteasome deubiquitinases (DUBs)

View related series

Cell Cycle/DNA Damage (2602) Deubiquitinase (86) ubiquitin specific peptidase 14 Inhibitor (3) Unfolded Protein Response (214)

Basic Description

Synonyms	4H-Azepin-4-one,3,5-bis[(4-fluoro-3-nitrophenyl)methylene]hexahydro-1-(1-oxo-2-propen-1-yl)-
Specifications & Purity	Moligand™, ≥99%
Biochemical and Physiological Mechanisms	VLX1570 is a competitive inhibitor of proteasome DUB activity, with an IC50 of ~10\u2009μM in vitro.
Storage Temp	Store at -20°C
Shipped In	Ice chest + Ice pads This product requires cold chain shipping. Ground and other economy services are not available.
Grade	Moligand™
Action Type	INHIBITOR
Mechanism of action	Inhibitor of ubiquitin specific peptidase 14
Product Description	Information VLX1570 VLX1570 is a competitive inhibitor of proteasome DUB activity, with an IC50 of ~10 μM in vitro. Targets DUB (Cell-free assay) ~10 μM In vitro VLX1570 is an analogue of b-AP15 that shows higher potency and improved solubility. VLX1570 preferentially inhibits proteasomal DUB activity while not inhibiting the activities of a panel of non-proteasomal DUBs. VLX1570 binds to and inhibits the activity of ubiquitin-specific protease-14 (USP14) with comparatively weaker inhibitory activity towards UCHL5 (ubiquitin-C-terminal hydrolase-5). Treatment of multiple myeloma cells with VLX1570 induces the accumulation of proteasome-bound high molecular weight polyubiquitin conjugates and an apoptotic response. VLX1570 induces the expression of the chaperone HSP70B′, the oxidative stress marker Hmox-1, and the ER stress marker XBP-1s. VLX1570 is retained in cells after removal of drug and that USP14 was engaged by drug 17\u2009hours after wash-out, as evidenced by thermal stabilization and persistent enzyme inhibition. In vivo VLX1570 is an inhibitor of proteasome DUB activity currently in clinical trials for relapsed multiple myeloma. Treatment with VLX1570 is found to lead to extended survival in xenograft models of multiple myeloma. The in vivo IC50 for inhibition of proteasome DUB activity and induction of apoptosis is <1\u2009μM, with multiple myeloma cells showing greater levels of sensitivity compared to other tumor types. The lower IC50 for activity in vivo is presumably due to rapid drug uptake and enrichment in cells. Cell Research(from reference) Cell lines：OPM-2\u2009MM cells Concentrations：0.5 μM Incubation Time：3 h

Taxonomic Classification

Taxonomy Tree

Kingdom Organic compounds
- Superclass Benzenoids
  - Class Benzene and substituted derivatives
    - Subclass Nitrobenzenes

Kingdom	Organic compounds
Superclass	Benzenoids
Class	Benzene and substituted derivatives
Subclass	Nitrobenzenes
Intermediate Tree Nodes	Not available
Direct Parent	Nitrobenzenes
Alternative Parents	Nitroaromatic compounds Fluorobenzenes Azepanes Aryl fluorides Tertiary carboxylic acid amides Acrylic acids and derivatives Cyclic ketones Propargyl-type 1,3-dipolar organic compounds Organic oxoazanium compounds Azacyclic compounds Organopnictogen compounds Organonitrogen compounds Organofluorides Organic oxides Hydrocarbon derivatives
Molecular Framework	Aromatic heteromonocyclic compounds
Substituents	Nitrobenzene - Nitroaromatic compound - Halobenzene - Fluorobenzene - Azepane - Aryl halide - Aryl fluoride - Acrylic acid or derivatives - Tertiary carboxylic acid amide - Organic nitro compound - Cyclic ketone - C-nitro compound - Ketone - Carboxamide group - Azacycle - Organoheterocyclic compound - Organic 1,3-dipolar compound - Propargyl-type 1,3-dipolar organic compound - Allyl-type 1,3-dipolar organic compound - Organic oxoazanium - Carboxylic acid derivative - Organic nitrogen compound - Organic oxygen compound - Organopnictogen compound - Organic oxide - Hydrocarbon derivative - Organooxygen compound - Organonitrogen compound - Organofluoride - Organohalogen compound - Carbonyl group - Aromatic heteromonocyclic compound
Description	This compound belongs to the class of organic compounds known as nitrobenzenes. These are compounds containing a nitrobenzene moiety, which consists of a benzene ring with a carbon bearing a nitro group.
External Descriptors	Not available
1. Djoumbou Feunang Y, Eisner R, Knox C, Chepelev L, Hastings J, Owen G, Fahy E, Steinbeck C, Subramanian S, Bolton E, Greiner R, and Wishart DS. ClassyFire: Automated Chemical Classification With A Comprehensive, Computable Taxonomy. Journal of Cheminformatics, 2016, 8:61. DOI: 10.1186/s13321-016-0174-y

Product Properties

ALogP	4.385
Rotatable Bond	5

Associated Targets(Human)

USP14 Tchem Ubiquitin carboxyl-terminal hydrolase 14 (0 Activities)

Discover Target: USP14

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Names and Identifiers

Pubchem Sid	504772904
Pubchem Sid Url	https://pubchem.ncbi.nlm.nih.gov/substance/504772904
IUPAC Name	(3Z,5Z)-3,5-bis[(4-fluoro-3-nitrophenyl)methylidene]-1-prop-2-enoylazepan-4-one
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-
InChIKey	SCKXBVLYWLLALY-CQRYCMKKSA-N
Smiles	C=CC(=O)N1CCC(=CC2=CC(=C(C=C2)F)[N+](=O)[O-])C(=O)C(=CC3=CC(=C(C=C3)F)[N+](=O)[O-])C1
PubChem CID	118989091
MeSH Entry Terms	VLX1570
Molecular Weight	469.39

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):

Analytical Chart:

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12 results found

Lot Number	Certificate Type	Date	Item
H2324066	Certificate of Analysis	Aug 08, 2023	V413963
H2324065	Certificate of Analysis	Aug 08, 2023	V413963
H2324203	Certificate of Analysis	Aug 08, 2023	V413963
H2324168	Certificate of Analysis	Aug 08, 2023	V413963
H2324212	Certificate of Analysis	Aug 08, 2023	V413963
H2324166	Certificate of Analysis	Aug 08, 2023	V413963
H2324184	Certificate of Analysis	Aug 08, 2023	V413963
H2324242	Certificate of Analysis	Aug 08, 2023	V413963
H2324208	Certificate of Analysis	Aug 08, 2023	V413963
H2324250	Certificate of Analysis	Aug 08, 2023	V413963
H2324067	Certificate of Analysis	Aug 08, 2023	V413963
H2324173	Certificate of Analysis	Aug 08, 2023	V413963

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Chemical and Physical Properties

Solubility	Solubility (25°C) In vitro DMSO: 93 mg/mL (198.12 mM); Water: Insoluble; Ethanol: Insoluble;
DMSO(mg / mL) Max Solubility	93
DMSO(mM) Max Solubility	198.1294872
Water(mg / mL) Max Solubility	＜1

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