1. Anti-infection Apoptosis NF-κB
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  3. Ciapavir

Ciapavir (SBI-0953294) is a HIV-1 latency-reversing agent. Ciapavir reverses latent HIV-1 reservoir in vitro and in vivo without inducing systemic T cell activation or broad cytokine release. Ciapavir degrades cIAP1 and activates non-canonical NF-κB pathway. Ciapavir can be used for the research of HIV-1 infection.

For research use only. We do not sell to patients.

Ciapavir

Ciapavir Chemical Structure

CAS No. : 2433895-70-4

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Description

Ciapavir (SBI-0953294) is a HIV-1 latency-reversing agent. Ciapavir reverses latent HIV-1 reservoir in vitro and in vivo without inducing systemic T cell activation or broad cytokine release. Ciapavir degrades cIAP1 and activates non-canonical NF-κB pathway. Ciapavir can be used for the research of HIV-1 infection[1].

IC50 & Target[1]

HIV-1

 

cIAP

 

In Vitro

Ciapavir (0.1-10000 nM; 48 h) mediates HIV-1 latency reversal in 2D10 Jurkat cells through activation of the non-canonical NF-κB pathway[1].
Ciapavir (1-10 μM; 24 h) does not trigger cytokine release or T cell activation in human PBMCs or resting CD4+ T cells at concentrations up to 10 μM[1].
Ciapavir (0.1-10000 nM; 48 h) synergizes with BET inhibitors JQ1 (HY-13030) and I-BET151 (HY-13235) to enhance HIV-1 latency reversal in 2D10 Jurkat cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Ciapavir (10-20 mg/kg; i.p.; single dose) demonstrates robust target engagement (cIAP1 degradation) in C57BL/6J mice without triggering significant cytokine release[1].
Ciapavir (10-20 mg/kg; i.p.; single dose) induces latent HIV-1 expression in antiretroviral therapy-treated BLT mice without overt immune activation[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: B6.129S-Rag2tm1Fwa Cd47tm1Fpl Il2rgtm1Wjl/J (male and female, 3 months old)[1]
Dosage: 10 mg/kg; 20 mg/kg
Administration: I.p., single dose
Result: Caused three of nine treated mice to exhibit increases in plasma HIV RNA 48 hours post-administration.
caused four of six mice in the 20 mg/kg group to show a significant increase in bone marrow HIV RNA.
Did not cause significant upregulation of CD69 in blood CD45+ cells or CD4+ T cells, or in bone marrow CD45+ cells.
Induced modest CD69 upregulation in bone marrow CD4+ T cells at 10 mg/kg but not 20 mg/kg.
Molecular Weight

1023.31

Formula

C54H70N8O8S2

CAS No.
SMILES

O=C([C@H]1N2[C@](SCC[C@@H](C2=O)NC([C@H](C)NC)=O)([H])CC1(C)C)N[C@@H](C3=CC=CC=C3C4)[C@@H]4OCC#CC#CCO[C@@H]5CC6=CC=CC=C6[C@@H]5NC([C@H]7N8[C@](SCC[C@@H](C8=O)NC([C@H](C)NC)=O)([H])CC7(C)C)=O

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  • 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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Ciapavir
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