Domatinostat tosylate

SKU: orb1302825

描述

研究领域

Cell Biology, Epigenetics & Chromatin, Molecular Biology

图片与验证

−

关键属性

−

CAS 号	1186222-89-8
MW	619.71
纯度	>99.99% (May vary between batches)
分子式	C₃₀H₂₉N₅O₆S₂
SMILES	Cc1ccc(cc1)S(O)(=O)=O.Cn1cc(cn1)-c1ccc(cc1)S(=O)(=O)n1ccc(\C=C\C(=O)Nc2ccccc2N)c1
靶点	HDAC,Apoptosis
溶解性	H2O:Insoluble;DMSO:50 mg/mL (80.68 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.23 mM)

生物活性

−

靶点 IC50	HDAC9:50 μM\|HDAC5:11.3 μM\|HDAC1:1.2 μM\|HDAC2:1.12 μM\|HDAC11:9.7 μM\|HDAC10:21 μM\|HDAC3:0.57 μM
体内	4SC-202 (i.g.) inhibits HT-29 xenograft growth in nude mice, and when combined with oxaliplatin, its activity is further strengthened.
体外	Domatinostat provokes apoptosis activation in CRC cells, while caspase inhibitors (z-VAD-CHO and z-DVED-CHO) significantly alleviate Domatinostat-exerted cytotoxicity in CRC cells. Meanwhile, Domatinostat induces dramatic G2-M arrest in CRC cells. Further studies show that AKT activation might be an important resistance factor of Domatinostat. Domatinostat-induced cytotoxicity is dramatically potentiated with serum starvation, AKT inhibition (by perifosine or MK-2206), or AKT1-shRNA knockdown in CRC cells. On the other hand, exogenous expression of constitutively active AKT1 (CA-AKT1) decreases the sensitivity by Domatinostat in HT-29 cells. Notably, Domatinostat, at a low concentration, enhances oxaliplatin-induced in vitro anti-CRC activity. Domatinostat obviously reduces the proliferation of all epithelial and mesenchymal UC cell lines (IC50: 0.15-0.51 μM), inhibits clonogenic growth and induces caspase activity. Domatinostat treatment induces potent cytotoxic and proliferation-inhibitory activities against established HCC cell lines (HepG2, HepB3, SMMC-7721) and patient-derived primary HCC cells. Domatinostat induces apoptosis signal-regulating kinase 1 (ASK1) activation, causing it translocation to mitochondria and physical association with Cyp-D.

储存与操作

−

储存	-20°C
有效期	12 months from date of receipt.
免责声明	For research use only

别名

−

Apoptosis, 4SC 202, 4SC 202 Tosylate, 4SC202, 4SC-202, 4SC202 Tosylate, Domatinostat, HDAC9, HDAC, HDAC1, HDAC10, HDAC2, HDAC11, HDAC3, HDAC5

相似产品

−

4SC-202 free base [orb1223678]
纯度：
>98% (HPLC)
CAS 号：
910462-43-0
MW:
447.51
分子式：
C??H??N?O?S
可选规格： 2 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg, 200 mg, 500 mg, 1 g

质量保证

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our 条款与条件和选购指南.

化合物标识

PubChem CID

44217246 ↗

关键属性

−

暂无计算属性。

实验方案信息

查看更多实验方案

纯度：	>98% (HPLC)
CAS 号：	910462-43-0
MW:	447.51
分子式：	C??H??N?O?S

Domatinostat tosylate

描述

研究领域

图片与验证

关键属性

生物活性

储存与操作

别名

相似产品

4SC-202 free base [orb1223678]

质量保证

化合物标识

关键属性

实验方案信息

可选规格