HC-056456

Modify Date: 2025-09-04 20:12:53

HC-056456 Structure
HC-056456 structure
Common Name HC-056456
CAS Number 7733-96-2 Molecular Weight 306.31700
Density N/A Boiling Point N/A
Molecular Formula C12H6N2O4S2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of HC-056456


HC-056456 is an effective but not perfectly-selective blocker of CatSper channels. The [Na+]i rise is slowed by HC-056456 (IC50~3 µM).

 Names

Name [5-oxido-4-(thiophene-2-carbonyl)-1,2,5-oxadiazol-5-ium-3-yl]-thiophen-2-ylmethanone
Synonym More Synonyms

 HC-056456 Biological Activity

Description HC-056456 is an effective but not perfectly-selective blocker of CatSper channels. The [Na+]i rise is slowed by HC-056456 (IC50~3 µM).
Related Catalog
Target

CatSper[1]

In Vitro HC-056456 similarly slows the rise of [Ca2+]i that is evoked by alkaline depolarization and reported by fura-2. HC-056456 also selectively and reversibly decreased CatSper currents recorded from patch-clamped sperm. HC-056456 produces a pharmacological phenocopy of the CatSper-null sperm. Acute application of HC-056456 causes rapid loss of flagellar waveform asymmetry from hyperactivated sperm, indicating that continued entry of Ca2+ through CatSper channels is required to maintain hyperactivation. HC-056456 selectively and reversibly blocks CatSper currents. The specificity and reversibility of the blockade of CatSper-dependent currents by HC-056456 is examined by using patch clamp recordings. The observed current is blocked slightly more than 50% by 20 µM HC-056456 (estimated IC50 near 15 µM). In concept, it remains possible that CatSper channel heterogeneity explains residual HC-056456-resistant current. The action of HC-056456 on KSper channels, the other major cation channel observed in patch-clamped sperm, is also examined. Subsequent application of 50 µM HC-056456 results in partial blockade of this current. For HC-056456 action on KSper an IC50 near 40 µM is estimated[1].
References

[1]. Carlson AE, et al. Pharmacological targeting of native CatSper channels reveals a required role in maintenance of sperm hyperactivation. PLoS One. 2009 Aug 31;4(8):e6844.

 Chemical & Physical Properties

Molecular Formula C12H6N2O4S2
Molecular Weight 306.31700
Exact Mass 305.97700
PSA 142.11000
LogP 2.68810
InChIKey RUQGCDMXFBOTMW-UHFFFAOYSA-N
SMILES O=C(c1cccs1)c1no[n+]([O-])c1C(=O)c1cccs1
Storage condition 2-8℃

 Synthetic Route

~57%

HC-056456 Structure

HC-056456

CAS#:7733-96-2

Literature: Espenbetov, A. A.; Struchkov, Yu. T.; Churkin, Yu. D.; Panfilova, L. V. J. Gen. Chem. USSR (Engl. Transl.), 1985 , vol. 55, # 7 p. 1565 - 1570,1392 - 1396

 Precursor & DownStream

Precursor  1

DownStream  0

 HC-056456Bioassay

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Name: Primary cell-based high-throughput screening assay for identification of compounds th...
Source: Johns Hopkins Ion Channel Center
Target: regulator of G-protein signaling 4 isoform 2 [Homo sapiens]
External Id: JHICC_RGS_Act_HTS
Name: Luminescence-based cell-based primary high throughput screening assay to identify ago...
Source: The Scripps Research Institute Molecular Screening Center
Target: mu-type opioid receptor isoform MOR-1 [Homo sapiens]
External Id: OPRM1-OPRD1_AG_LUMI_1536_1X%ACT PRUN
Name: Inhibition of SARS-CoV-2 3CL-Pro proteolytic cleavage of a dual-labeled substrate by ...
Source: ChEMBL
Target: Replicase polyprotein 1ab
External Id: CHEMBL5303714
Name: Inhibition of SARS-CoV-2 3CL-Pro proteolytic cleavage of a dual-labeled substrate by ...
Source: ChEMBL
Target: Replicase polyprotein 1ab
External Id: CHEMBL5303713
Name: Fluorescence-based cell-based primary high throughput screening assay to identify ago...
Source: The Scripps Research Institute Molecular Screening Center
Target: muscarinic acetylcholine receptor M1 [Homo sapiens]
External Id: CHRM1_AG_FLUO8_1536_1X%ACT PRUN
Name: uHTS identification of small molecule activators of the adaptive arm of the Unfolded ...
Source: Burnham Center for Chemical Genomics
Target: N/A
External Id: BCCG-A405-UPR-XBP1-PrimaryAgonist-Assay
Name: A screen for compounds that inhibit the activity of LtaS in Staphylococcus aureus
Source: ICCB-Longwood/NSRB Screening Facility, Harvard Medical School
External Id: HMS979
Name: High throughput fluorescence intensity-based biochemical assay to screen for small mo...
Source: University of Pittsburgh Molecular Library Screening Center
Target: furin (paired basic amino acid cleaving enzyme), isoform CRA_a [Homo sapiens]
External Id: MH080376 Biochemical HTS for Inhibitors of the Proprotein Convertase Furin.
Name: Fluorescence polarization to screen for inhibitor that competite the binding of FadD2...
Source: Broad Institute
Target: FATTY-ACID-CoA LIGASE FADD28 (FATTY-ACID-CoA SYNTHETASE)
External Id: 2147-01_Inhibitor_SinglePoint_HTS_Activity
Name: qHTS of TDP-43 Inhibitors: NCGC Sytravon Library Screen
Source: NCGC
External Id: tdp43-p2-repeat
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 Synonyms

3,4-Bis<2-thienylcarbonyl>furazan-oxid
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