Home Microbiology Reverse Transcriptase inhibitor - CRISPR/Cas9 modulator Zidovudine For research use only.

Zidovudine

Synonyms: Azidothymidine, NSC 602670

Zidovudine (ZDV, Azidothymidine, NSC 602670) is a nucleoside analogue reverse transcriptase inhibitor, used to treat HIV. It could decrease the HDR efficiency and decrease CRISPR-mediated sequence-specific genome knockin events while increaseing knockout efficiency.

Zidovudine Chemical Structure

Zidovudine Chemical Structure

CAS: 30516-87-1

Selleck's Zidovudine has been cited by 18 publications

Purity & Quality Control

Batch: Purity: 100%
100

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human C8166 cells Function assay Antiviral activity against Human immunodeficiency virus 1 infected in human C8166 cells assessed as inhibition of virus-induced cytopathic effect, EC50=4e-06 μM 21534540
PBMC Function assay 1 μM Antiviral activity against HIV1 TEKI replication in PBMC at 1 uM, IC50=0.00014 μM 16420027
human H9 cells Function assay 6 days Antiviral activity against Human immunodeficiency virus 1 3B infected in human H9 cells infected with 6.25 uL of virus stock assessed as expression of p24 antigen after 6 days postinfection by ELISA, IC50=0.3 nM 20086149
AA5 cells Function assay Antiviral activity against of Human immunodeficiency virus 1 3B infected in AA5 cells infected with 1.56 uL of virus stock assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay, IC50=0.3 nM 20086149
CEM cells Function assay Concentration of the drug resulting in 50% reduction of the viral cytopathic effect against HIV-1 replication in CEM cells, EC50=0.32 nM 2153206
MT4 cells Function assay 4 days Antiviral activity against HIV1 3B assessed as inhibition of virus-induced cytopathogenicity in MT4 cells after 4 days by MTT assay, EC50=0.7 nM 17964796
human MT2 cells Function assay 1 h Antiviral activity against HIV1 subtype B-3B infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA, EC50=1.2 nM 18316521
C8166 cells Function assay Inhibition of HIV1-3B replication in C8166 cells, EC50=1.9 nM 16279773
CEM-SS cell Function assay Inhibitory activity against the HIV-1-induced cytopathic effect in CEM-SS cell line, IC50=0.002 μM 7650678
PBLs Function assay Antiviral activity against subtype isolate G strain in PBLs (peripheral blood lymphocytes), IC50=0.002 μM 11708913
human lymphocyte CEM/0 cell line Function assay Anti HIV-1 activity in human lymphocyte CEM/0 cell line, EC50=0.003 μM 8478904
Jurkat cell Function assay Inhibitory concentration against HIV-1 infected Jurkat cell lines, IC50=0.01 μM 7837220
human H9 cells Cytotoxicity assay 6 days Cytotoxicity against human H9 cells after 6 days by MTT assay, EC50=0.01 μM 20846868
C3H/3T3 cells Function assay Concentration of compound required to inhibit HIV-1 induced cytopathogenicity of MSV-induced transformation of C3H/3T3 cells by 50%, EC50=0.02 μM 2016718
U937 cells Function assay Effective concentration required for antiviral activity against Macrophage cell line of U937 cells of Human by XTT assay, EC50=0.03 μM 7932526
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Biological Activity

Description Zidovudine (ZDV, Azidothymidine, NSC 602670) is a nucleoside analogue reverse transcriptase inhibitor, used to treat HIV. It could decrease the HDR efficiency and decrease CRISPR-mediated sequence-specific genome knockin events while increaseing knockout efficiency.
Targets
Reverse transcriptase [1]
In vitro
In vitro

Zidovudine pretreatment has potent anti-HIV-1 activity in the newly infected T and monocytic cells but not in chronically infected cells. [1] Inhibition of reverse transcription by Zidovudine decreases p24 antigen levels modestly, decreased HIV-1 gag by 19-fold, and inhibits detection of 2-LTR HIV-1 DNA. [2] Zidovudine and dideoxynucleosides deplete wild-type mitochondrial DNA levels and increase deletedmitochondrial DNA levels in cultured Kearns-Sayre syndrome fibroblasts. [3] Zidovudine (AZT, 0.1-50 mM) has a concentration dependent suppressive effect on the growth of granulocyte-monocyte colony forming unit (CFU-GM) derived colonies. Zidovudine exposure also induces a concentration dependent suppressive effect (35-90%) on GM-CSF receptor type alpha (GM-CSFR alpha) gene expression. Zidovudine causes a much lower decrease (15-22%) on the IL-3 receptor type alpha (IL-3R alpha) message level, and has an insignificant effect on glyceraldehyde 3-phosphate dehydrogenase (GAPDH) and c-myc message levels. [4] Zidovudine causes a concentration-dependent inhibition in the levels of the mRNA of Epo receptors and c-fos, whereas the level of c-myc mRNA is unaffected. Zidovudine also inhibits protein kinase C (PKC) activity in a concentration- and time-dependent manner, causing 50% inhibition at 10 mM within 3 hours. Zidovudine-induced down-regulation of Epo receptors and c-fos expression coupled with inhibition of Epo receptor-mediated signal transduction through PKC are significant contributory factors to AZT-induced erythroid toxicity. [5] Zidovudine could decrease the HDR efficiency. It decrease CRISPR-mediated sequence-specific genome knockin events while increases knockout efficiency[6] .
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03991013 Completed HIV Infections University of Cape Town|Wellcome Trust|Médecins Sans Frontières Belgium August 8 2019 Phase 2
NCT03642704 Completed Mother to Child HIV Transmission ANRS Emerging Infectious Diseases February 22 2017 Phase 4

Chemical lnformation & Solubility

Molecular Weight 267.24 Formula

C10H13N5O4
CAS No. 30516-87-1 SDF Download Zidovudine SDF
Smiles CC1=CN(C(=O)NC1=O)C2CC(C(O2)CO)N=[N+]=[N-]
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 53 mg/mL ( (198.32 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 53 mg/mL

Ethanol : 18 mg/mL


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

Question 1:
Do you happen to have any information regarding the half-life of AZT？

Answer:
The Half-life of S2579 in human is available (http://www.rxlist.com/retrovir-drug/clinical-pharmacology.htm), about 0.5-3 hours in adult subjects.

Reverse Transcriptase Signaling Pathway Map

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