Chemical Structure : B029-2
CAS No.:
2379410-19-0
B029-2
(SYY-B029-2)
Catalog No.: PC-28014Not For Human Use, Lab Use Only.
B029-2 (SYY-B029-2) is a potent p300/CBP histone acetyltransferase (HAT) inhibitor with IC50 of 0.49/7.1 nM for p300/CBP rspectively, shows anti-proliferation on ovarian cancer cell line OVCAR-3 with IC50 of 153 nM.
Bulk size, bulk discount!
E-mail: sales@probechem.com
Tech Support: tech@probechem.com
Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
B029-2 (SYY-B029-2) is a potent p300/CBP histone acetyltransferase (HAT) inhibitor with IC50 of 0.49/7.1 nM for p300/CBP rspectively, shows anti-proliferation on ovarian cancer cell line OVCAR-3 with IC50 of 153 nM.
B029-2 shows no activity against HATs including p300, GCN5, NatD, PCAF, KAT7 and MOF, as long as some Non-HATs histone modification enzyme including JMJD2A, LSD1, HDAC1 and HDAC2.
B029-2 strongly inhibits the activity of p300/CBP in ovarian cancer cell lines and affect downstream signaling pathways.
B029-2 (30 mg/kg, qd). significantly enhances the antitumor effect in OVCAR-3 xenograft models.
B029-2 specifically decreased H3K18Ac and H3K27Ac and displayed significant antitumor effects in HCC cells in vitro and in vivo.
Physicochemical Properties
|
M.Wt
|
522.53
|
|
Formula
|
C27H27FN4O6
|
|
Appearance
|
Solid
|
|
CAS No.
|
|
|
Storage
|
- Solide Powder
-
-20°C 12 Months; 4°C 6 Months
|
- In Solvent
-
-80°C 6 Months; -20°C 6 Months
|
|
Shipping
|
|
|
Solubility
|
10 mM in DMSO
|
|
Chemical Name/SMILES
|
1-((R)-3'-(2-((R)-3-cyclopropyl-7-fluoro-2,3-dihydrobenzo[f][1,4]oxazepin-4(5H)-yl)-2-oxoethyl)-2',4'-dioxo-2,3-dihydrospiro[indene-1,5'-oxazolidin]-5-yl)-3-methylurea
|
References
1. Cai LY, et al. Cancer Res. 2021 Feb 15;81(4):860-872.
2. Hong Ding, et al. Bioorg Med Chem. 2021 Dec 15:52:116512.
Contact Us
sales@probechem.com
