NI-57
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 250mg | $1450 | Check With Us |
| 500mg | $2200 | Check With Us |
| 1g | $3300 | Check With Us |
: Cat #: V26460 CAS #: 1883548-89-7 Purity ≥ 99%
Description: NI-57 is a potent inhibitor of the bromodomains of BRPF proteins that binds to BRPF1B, BRPF2, and BRPF3 with Kd values of 31, 108, and 408 nM, respectively
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| Molecular Weight (MW) | 383.42 |
|---|---|
| Molecular Formula | C19H17N3O4S |
| CAS No. | 1883548-89-7 |
| SMILES Code | O=S(C1=CC=C(C#N)C=C1OC)(NC2=CC3=C(N(C)C(C(C)=C3)=O)C=C2)=O |
| Synonyms | NI-57; NI 57; NI57 |
| Protocol | In Vitro | NI-57 is an inhibitor of bromodomain and plant homeodomain finger-containing (BRPF), with IC50s of 3.1, 46 and 140 nM for BRPF1, BRPF2 (BRD1) and BRPF3, respectively. NI-57 binds the BRD of BRPF1 with a Kd of 31 ± 2 nM, BRD1 with a Kd of 110 ± 13 nM, and BRPF3 with a Kd of 410 ± 47 nM, whereas binding to BRD9 is weaker (Kd 1000 ± 130 nM) measured by isothermal titration calorimetry. NI-57 shows less active effect on BRD9 (IC50, 520 nM) and BRD4 (BD1) (IC50, 3700 nM), TRIM24 (IC50, 1600 nM). NI-57 also inhibits BRPF BRDs in the nucleus, but shows little effect on the proliferation of many cancer cell lines with GI50s of 10.4 μM (NCI-H1703 cells), 14.7 μM (DMS114), 15.6 μM (HRA-19), and 16.6 μM (RERF-LC-Sq1). Furthermore, Inhibition on BRPF1 of NI-57 (10 μM) reduces the gene expression of CCL-22 by 27.7 ± 9.4%. |
|---|---|---|
| In Vivo | NI-57 has favorable oral bioavailability in mice. |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.6081 mL | 13.0405 mL | 26.0811 mL | 52.1621 mL |
| 5mM | 0.5216 mL | 2.6081 mL | 5.2162 mL | 10.4324 mL |
| 10mM | 0.2608 mL | 1.3041 mL | 2.6081 mL | 5.2162 mL |
| 20mM | 0.1304 mL | 0.6520 mL | 1.3041 mL | 2.6081 mL |
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