TP-472 是一种选择性的 BRD9/7 抑制剂，对 BRD9 和 BRD7 作用的 K_d 值分别为 33 nM 和 340 nM。TP-472 对 BRD9 的选择性比 BRD7 以外的其他溴结构域家族成员高 30 倍以上。TP-472 诱导黑色素瘤细胞凋亡 (apoptosis)。

TP-472 is a selective BRD9/7 inhibitor, with K d s of 33 nM and 340 nM for BRD9 and BRD7, respectively. TP-472 exhibits >30-fold selectivity for BRD9 over other bromodomain family members except BRD7. TP-472 induces apoptosis of melanoma cells.

Solid

BRD9 33 nM (Kd) BRD7 0.34 μM (Kd)

TP-472 (1 μM, 3 μM; 24-216 hours) yields concentration-dependent growth defects in ESCs.
TP-472 (0.1-10 μM; 24 h) effectively inhibits the growth of both the BRAF mutant melanoma cell lines at 5 and 10 μM concentrations.
TP-472 (for 2 weeks) also strongly inhibits the long-term survival of multiple melanoma cell lines (M14, SKMEL-28, A375, and A2058) at concentrations of 5 and 10 μM.
TP-472 (5-10 μM; 24 h) treatment downregulates genes encoding various extracellular matrix (ECM) proteins, including integrins, collagens, and fibronectins in A375 cells.
TP-472 (0.1-10 μM; 24 h) results in the upregulation of pro-apoptotic genes (BAX, MDM2, CDKN1A) in A375 cells.
has not independently confirmed the accuracy of these methods. They are for reference only.

TP-472 (20 mg/kg; i.p.; three times a week; for 5 weeks) significantly inhibits the subcutaneous tumor growth in melanoma xenograft mouse model. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Moustakim M, et al. Chemical probes and inhibitors of bromodomains outside the BET family. Medchemcomm. 2016 Dec 7;7(12):2246-2264.
[2]. Gatchalian J, et al. A non-canonical BRD9-containing BAF chromatin remodeling complex regulates naive pluripotency in mouse embryonic stem cells. Nat Commun. 2018 Dec 3;9(1):5139.

In Vitro: DMSO : 100 mg/mL (299.96 mM; ultrasonic and warming and heat to 60°C)配制储备液