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Chemical Structure : BI 224436
Catalog No.: PC-62482Not For Human Use, Lab Use Only.
BI 224436 (BI-224436) is a specific small molecule HIV-1 non-catalytic-site integrase inhibitor (NCINI) with IC50 of 15 nM in LTR 3'-processing assays.
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BI 224436 (BI-224436) is a specific small molecule HIV-1 non-catalytic-site integrase inhibitor (NCINI) with IC50 of 15 nM in LTR 3'-processing assays.
BI 224436 displayed minimal inhibition of the integrase strand transfer enzymatic activity with a mean IC50 of >50 uM.
BI 224436 inhibits both the LTR 3′-processing enzymatic activity and the integrase-LEDGF interaction with equivalent potencies
BI 224436 exhibited EC50s of 7.2 nM, 14 nM, and 15 nM observed for HXB2, NL4.3, and BaL integrase-containing viruses, respectively, in PBMCs.
BI 224436 also has a low, 2.1-fold decrease in antiviral potency in the presence of 50% human serum and, by virtue of a steep dose-response curve slope, exhibits serum-shifted EC95 values ranging between 22 and 75 nM.
BI 224436 retains full antiviral activity against recombinant viruses encoding INSTI resistance substitutions N155S, Q148H, and E92Q.
BI 224436 displays an additive effect in combination with most approved antiretrovirals in cellular antiviral assays, including INSTIs.
BI 224436 is the first NCINI to advance into a phase Ia clinical trial.
| M.Wt | 391.467 | |
| Formula | C24H25NO4 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Fader LD, et al. ACS Med Chem Lett. 2014 Jan 22;5(4):422-7.
2. Fenwick C, et al. Antimicrob Agents Chemother. 2014 Jun;58(6):3233-44.
3. Demeulemeester J, et al. Expert Opin Ther Pat. 2014 Jun;24(6):609-32.
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