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Table 1 Activity, CNS penetrance, and concentrations of LRA and positive controls

From: Contrasting effect of the latency-reversing agents bryostatin-1 and JQ1 on astrocyte-mediated neuroinflammation and brain neutrophil invasion

Compounds (activity) CNS penetrance [4] Concentrations used in our study HIV-1 reactivating concentrations in vitro Plasmatic concentrationsa
Bryostatin-1 (PKC modulator) ++ 25 nM 0.25–100 nM [29] 0.05 nMb [28]
JQ1 (BRDi) ++ 0.5 μM 0.5 μM [53] ND
SAHA (HDACi) +++ 1 μM 0.1–10 μM [53,54,55] 1 μM [56, 57]
HMBA (Tat mimetic) ++ 1 mM 1–5 mM [58, 59] 0.0019 mM [60]
Disulfiram (Akt signaller) +++ 1 μM 0.1–10 μM [53, 61, 62] 0.2 μM [63] 2 μM [64]
Bix-01294 (HMTi) ND 1 μM 1–10 μM [65] ND
Positive controls: poly(I:C) Pam3Csk4   30 μg/mL 10 μg/mL   
  1. PKC protein kinase C, BRDi bromodomain inhibitor, SAHA suberoylanilide hydroxamide acid, HDACi histone deacetylase inhibitor, HMBA hexamethylene bisacetamide, HMTi histone methyltransferase inhibitor, TLR Toll-like receptor, poly(I:C) polyinosinic/polycytidylic acid, ++/+++ good/very good penetration, ND not determined
  2. aMaximum in vivo plasma concentration in humans
  3. bNo HIV-1 reactivation at this low in vivo plasma concentration in humans