1. Anti-infection
  2. HIV
  3. HIV-1 inhibitor-6

HIV-1 inhibitor-6 (compound 9), a diheteroarylamide-based compound, is a potent HIV-1 pre-mRNA alternative splicing inhibitor. HIV-1 inhibitor-6 blocks HIV replication. HIV-1 inhibitor-6 is active against wild-type HIV-1IIIB (subtype B, X4-tropic) and HIV-1 97USSN54 (subtype A, R5-tropic) with EC50s of 0.6 μM and 0.9 μM, respectively. HIV-1 inhibitor-6 inhibits HIV strains resistant to agents targeting HIV reverse transcriptase, protease, integrase, and coreceptor CCR5 with EC50s ranging from 0.9 to 1.5 μM.

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HIV-1 inhibitor-6 Chemical Structure

HIV-1 inhibitor-6 Chemical Structure

CAS No. : 1821309-39-0

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Based on 1 publication(s) in Google Scholar

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1 Publications Citing Use of MCE HIV-1 inhibitor-6

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Description

HIV-1 inhibitor-6 (compound 9), a diheteroarylamide-based compound, is a potent HIV-1 pre-mRNA alternative splicing inhibitor. HIV-1 inhibitor-6 blocks HIV replication. HIV-1 inhibitor-6 is active against wild-type HIV-1IIIB (subtype B, X4-tropic) and HIV-1 97USSN54 (subtype A, R5-tropic) with EC50s of 0.6 μM and 0.9 μM, respectively. HIV-1 inhibitor-6 inhibits HIV strains resistant to agents targeting HIV reverse transcriptase, protease, integrase, and coreceptor CCR5 with EC50s ranging from 0.9 to 1.5 μM[1].

IC50 & Target[1]

X4 HIV-1 (IIIB)

0.6 μM (EC50)

R5 HIV-1

0.9 μM (EC50)

Cellular Effect
Cell Line Type Value Description References
CCRF-CEM CC50
> 100 μM
Compound: 9; 1C8
Cytotoxicity against GFP-positive human CEM cells expressing CD4+,CXCR4 and CCR5 assessed as cell viability at after 24 hrs by Guava viacount assay
Cytotoxicity against GFP-positive human CEM cells expressing CD4+,CXCR4 and CCR5 assessed as cell viability at after 24 hrs by Guava viacount assay
[PMID: 26878150]
CCRF-CEM EC50
0.6 μM
Compound: 9; 1C8
Antiviral activity against subtype B X4 tropic HIV1 3B infected in GFP-positive human CEM cells expressing CD4+,CXCR4 and CCR5 after 3 days
Antiviral activity against subtype B X4 tropic HIV1 3B infected in GFP-positive human CEM cells expressing CD4+,CXCR4 and CCR5 after 3 days
[PMID: 26878150]
CCRF-CEM EC50
0.9 μM
Compound: 9; 1C8
Antiviral activity against subtype A R5 tropic HIV1 97USSN54 infected in GFP-positive human CEM cells expressing CD4+,CXCR4 and CCR5 after 3 days
Antiviral activity against subtype A R5 tropic HIV1 97USSN54 infected in GFP-positive human CEM cells expressing CD4+,CXCR4 and CCR5 after 3 days
[PMID: 26878150]
CCRF-CEM EC50
0.9 μM
Compound: 9; 1C8
Antiviral activity against maraviroc-resistant HIV1 BAL R5 harboring envelop V3 A19T/L20F/T22A/E25D/126V mutant infected in GFP-positive human CEM cells expressing CD4+,CXCR4 and CCR5 after 3 days
Antiviral activity against maraviroc-resistant HIV1 BAL R5 harboring envelop V3 A19T/L20F/T22A/E25D/126V mutant infected in GFP-positive human CEM cells expressing CD4+,CXCR4 and CCR5 after 3 days
[PMID: 26878150]
CCRF-CEM EC50
1.3 μM
Compound: 9; 1C8
Antiviral activity against NNRTI-resistance HIV1 E00443 harboring reverse transcriptase D67N/K70R/Y115F/Q151M/M184V/K219Q mutant infected in GFP-positive human CEM cells expressing CD4+,CXCR4 and CCR5 after 3 days
Antiviral activity against NNRTI-resistance HIV1 E00443 harboring reverse transcriptase D67N/K70R/Y115F/Q151M/M184V/K219Q mutant infected in GFP-positive human CEM cells expressing CD4+,CXCR4 and CCR5 after 3 days
[PMID: 26878150]
CCRF-CEM EC50
1.4 μM
Compound: 9; 1C8
Antiviral activity against PI-resistant HIV1 isolate 2948 harboring protease G48V/L90M mutant infected in GFP-positive human CEM cells expressing CD4+,CXCR4 and CCR5 after 3 days
Antiviral activity against PI-resistant HIV1 isolate 2948 harboring protease G48V/L90M mutant infected in GFP-positive human CEM cells expressing CD4+,CXCR4 and CCR5 after 3 days
[PMID: 26878150]
CCRF-CEM EC50
1.5 μM
Compound: 9; 1C8
Antiviral activity against INI-resistant HIV1 isolate 11845 harboring integrase G140S/Q148H mutant infected in GFP-positive human CEM cells expressing CD4+,CXCR4 and CCR5 after 3 days
Antiviral activity against INI-resistant HIV1 isolate 11845 harboring integrase G140S/Q148H mutant infected in GFP-positive human CEM cells expressing CD4+,CXCR4 and CCR5 after 3 days
[PMID: 26878150]
Molecular Weight

330.32

Formula

C14H10N4O4S

CAS No.
Appearance

Solid

Color

Yellow to orange

SMILES

O=C(C1=CN(C)C=CC1=O)NC2=NSC3=C2C=C([N+]([O-])=O)C=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 3.33 mg/mL (10.08 mM; ultrasonic and warming and heat to 80°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0274 mL 15.1368 mL 30.2737 mL
5 mM 0.6055 mL 3.0274 mL 6.0547 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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This equation is commonly abbreviated as: C1V1 = C2V2

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.0274 mL 15.1368 mL 30.2737 mL 75.6842 mL
5 mM 0.6055 mL 3.0274 mL 6.0547 mL 15.1368 mL
10 mM 0.3027 mL 1.5137 mL 3.0274 mL 7.5684 mL
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HIV-1 inhibitor-6 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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HIV-1 inhibitor-6
Cat. No.:
HY-134851
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