BI-9564

  Cat. No.:  DC9888   Featured
Chemical Structure
1883429-22-8
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Field of application
BI-9564 is a selective, and cell-permeable BRD9 BD inhibitor, with Kd of 5.9 nM for BRD9, and IC50 of > 100 μM for BET family.
Cas No.: 1883429-22-8
Chemical Name: 4-[4-[(Dimethylamino)methyl]-2,5-Dimethoxy-Phenyl]-2-Methyl-2,7-Naphthyridin-1-One
Synonyms: BI-9564;BI 9564;4-(4-Dimethylaminomethyl-2,5-dimethoxy-phenyl)-2-methyl-2H-[2,7]naphthyridin-1-one;4-[4-[(Dimethylamino)methyl]-2,5-dimethoxyphenyl]-2-methyl-2,7-naphthyridin-1-one;GTPL8950;4-(4-((dimethylamino)methyl)-2,5-dimethoxyphenyl)-2-methyl-2,7-naphthyridin-1(2H)-one;4-[4-[(Dimethylamino)methyl]-2,5-Dimethoxy-Phenyl]-2-Methyl-2,7-Naphthyridin-1-One;4-[4-[(Dimethylamino)methyl]-2,5-dimethoxyphenyl]-2-methyl-1,2-dihydro-2,7-naphthyridin-1-one;4-{4-[(dimethylamino)methyl]-2,5-dimethoxyphenyl}-2-methyl-1,2-dihydro-2,7-naphthyridin-1-one;5U6;BCP17135;BDBM50183449;BI9564;s8113
SMILES: O(C([H])([H])[H])C1C([H])=C(C(=C([H])C=1C1=C([H])N(C([H])([H])[H])C(C2C([H])=NC([H])=C([H])C1=2)=O)OC([H])([H])[H])C([H])([H])N(C([H])([H])[H])C([H])([H])[H]
Formula: C20H23N3O3
M.Wt: 353.4149
Description: BI-9564 is a selective, and cell-permeable BRD9 BD inhibitor, with Kd of 5.9 nM for BRD9, and IC50 of > 100 μM for BET family.
In Vivo: BI-9564 (180 mg/kg, p.o.) shows attractive ADME/PK profiles for in vivo proof-of-concept studies. BI-9564 results in a modest but significant additional survival benefit of 2 days compared to survival of the control group in a xenograft model of human AML[1].
In Vitro: BI-9564 (<5 μM) shows no activity against 324 kinases, and at 10 μM, an inhibition >40% is observed for only 2 out of 55 GPCRs. BI-9564 has antiproliferative effect on human acute myeloid eosinophilic leukemia cell line EOL-1, with EC50 of 800 nM[1]. BI-9564 shows Kd of 73 nM for BRD7, and is >10-fold more selective for BRD9 over the highly homologues bromodomain BRD7, which has been implied as a tumor suppressor and is down-regulated in cancer cells[2].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
DC70466 GSK549 GSK549 (GSK-549) is a potent, highly selective, BD2 domain-selective BET inhibitor with pIC50 of 7.8 (BRD4 BD2), 1150-fold selectivity over BD1.
DC11261 ZL0420 ZL0420 is a potent, highly selective BRD4 inhibitor with IC50 of 27 and 32 nM for BRD4-BD1 and BRD4-BD2, respectively.
DC8261 (-)-JQ-1 The (-)-JQ1 stereoisomer has no appreciable affinity to BET bromodomains,it is the negative control of +JQ-1.
DC8320 RVX-208 RVX-208(RVX 000222) is a small molecule that increases apolipoprotein A-I and high-density lipoprotein cholesterol in vitro and in vivo; is a BET bromodomain antagonist.
DC10786 PLX51107 PLX51107 is a novel BET inhibitor with a unique binding mode in the acetylated lysine binding pocket of BRD4 that differentiates it from other compounds under investigation.
DC8291 PFI-4 PFI-4 is a potent and selective BRPF1 bromodomain inhibitor (IC50 = 80 nM).
DC7649 PFI-3 PFI-3 is a novel potent, selective and cell permeable inhibitor of SMARCA4 and PB1(5) bromodomains with IC50 ~ 89 nM and 48 nM respectively.
DC9305 PF-CBP1(PF-06670910) hydrochloride PF-CBP1 is potent and highly-selective inhibitor of the bromodomain of CREB binding protein (CBP BRD) that down regulates targets of CBP in macrophages primary neurons.
DC7850 OF-1 OF-1 is a potent inhibitor of BRPF1B and BRPF2 bromodomain with Kd of 100 nM and 500 nM, respectively.
DC9758 NI-57 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, as determined by isothermal titration calorimetry.
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