GNE-049

Name: GNE-049
Brand: TargetMol
SKU: T15397
Price: 278 USD
Availability: InStock
Rating: 4.5 (1 reviews)

产品编号 T15397Cas号 1936421-41-8

GNE-049 is a highly potent and selective inhibitor of CBP (IC50: 1.1 nM in TR-FRET assay). GNE-049 also inhibits BRET and BRD4(1) (IC50s: 12 nM and 4200 nM, respectively).

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GNE-049

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产品编号 T15397Cas号 1936421-41-8

GNE-049 is a highly potent and selective inhibitor of CBP (IC50: 1.1 nM in TR-FRET assay). GNE-049 also inhibits BRET and BRD4(1) (IC50s: 12 nM and 4200 nM, respectively).

规格	价格	库存
2 mg	¥ 3,630	5日内发货
5 mg	¥ 4,570	5日内发货
25 mg	¥ 13,900	8-10周
50 mg	¥ 18,300	8-10周
100 mg	¥ 23,500	8-10周
1 mL x 10 mM (in DMSO)	¥ 5,130	5日内发货

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产品介绍

生物活性

产品描述	GNE-049 is a highly potent and selective inhibitor of CBP (IC50: 1.1 nM in TR-FRET assay). GNE-049 also inhibits BRET and BRD4(1) (IC50s: 12 nM and 4200 nM, respectively).
靶点活性	CBP:1.1 nM, BRET:12 nM, BRD41:4200 nM
体外活性	GNE-049 inhibits the expression of MYC (EC50: 14 nM). GNE-049 has excellent potency in the BRET cellular assay and, in an orthogonal measure of the target engagement. GNE-049 is selected for further profiling as it has the best balance of liver microsomes (LM) stability, selectivity, and cellular potency.
体内活性	GNE-049 shows acceptable PK in mouse, rat, dog, and monkey. GNE-049 is further evaluated in a rat single dose (30-250 mg/kg QD) toxicokinetic study. GNE-049 is selective for CBP/P300 and, importantly, quite selective (3820-fold) over BRD4(1), which revealed from the Determination of potency versus a selection of bromodomains. Furthermore, at the 250 mg/kg dose level, the ratio of the unbound drug concentration in the brain to unbound drug concentration in plasma (Kp,uu) 3 h post-dose is determined to be 0.43, indicating that GNE-049 is penetrating into the CNS and potentially resulting in the observed toxicity.

化学信息

分子量	510.58
分子式	C₂₇H₃₂F₂N₆O₂
CAS No.	1936421-41-8

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

溶解度信息

DMSO: 100 mg/mL (195.86 mM), Sonication is recommended.

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.9586 mL	9.7928 mL	19.5856 mL	97.9278 mL
5 mM	0.3917 mL	1.9586 mL	3.9171 mL	19.5856 mL
10 mM	0.1959 mL	0.9793 mL	1.9586 mL	9.7928 mL
20 mM	0.0979 mL	0.4896 mL	0.9793 mL	4.8964 mL
50 mM	0.0392 mL	0.1959 mL	0.3917 mL	1.9586 mL
100 mM	0.0196 mL	0.0979 mL	0.1959 mL	0.9793 mL