This probe is available from Tocris, Cayman Chemical and Sigma.
Its negative control (TP-472N) is available for purchase from Tocris and Sigma.
For any inquiries please contact firstname.lastname@example.org.
The bromodomain containing protein 9 (BRD9) has been reported as a component of the switch/sucrose non-fermentable (SWI/SNF) brahma-related gene 1-associated factor (BAF) complex, which plays a key role in chromatin remodelling and transcription control  although the precise biological role is unknown. The highly homologous bromodomain containing protein 7 (BRD7) is a component of the SWI/SNF polybromo-associated BAF (PBAF) complex and has been proposed as a tumor suppressor .
In a collaborative effort Takeda and the SGC have identified and characterised TP-472 as a BRD9/7 probe. This molecule is of a different chemotype to the BRD9/7 probes previously available, has a structurally similar negative control available (TP-472N), has a good PK profile and is suitable for in vivo applications and is synthetically tractable.
TP-472 has excellent potency (BRD9 KD 33nM; BRD7 340nM by ITC), selectivity >30 fold over all other bromodomain family members except BRD7 and is cell active (EC50 320 nM in a BRD9 NanoBRET assay). The negative control TP472N is inactive against other bromodomains (>20uM against BRD9)
Physical and chemical properties for TP-472
No. of chiral centres
No. of rotatable bonds
No. of hydrogen bond acceptors
No. of hydrogen bond donors
Physical and chemical properties for TP-472N (Negative Control)
Selectivity beyond target family
TP-472 and TP-472N were screened in the Eurofins CEREP Diversity Profile to measure binding to a range of Receptors, Ion Channels and enzymes @10 uM. The Inhibition as the mean % of control is shown below, results showing an inhibition or stimulation lower than 50% are considered to represent significant effects. TP-472 showed binding to Adenosine A1 receptor (14%), Benzodiazepine receptor (47%), PDE2A1 (h) (25%), PDE3A (h) (48%) and PDE4D2 (h) (28%). TP-472N showed binding to A1 receptor (35%), A3 receptor (23%), Melatonin receptor MT1 (47%) and Cl- channel (GABA-gated) (20%).
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