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17374-26-4

中文名稱 4,5,6,7-四溴-1H-苯并三唑
英文名稱 4,5,6,7-TETRABROMOBENZOTRIAZOLE
CAS 17374-26-4
分子式 C6HBr4N3
分子量 434.71
MOL 文件 17374-26-4.mol
更新日期 2024/12/13 09:51:39
17374-26-4 結(jié)構(gòu)式 17374-26-4 結(jié)構(gòu)式

基本信息

中文別名
7-四溴苯并三唑
4,5,6,7-四溴苯并三唑
4,5,6,7-四溴苯基三唑
4,5,6,7-四溴-1H-苯并三唑
TBB(4,5,6,7-四溴-1H-苯并三唑)
英文別名
TBB
TBBT
NSC 231634
CK2 INHIBITOR
TBB(NSC 231634)
TBB (enzyMe inhibitor)
4,5,6,7-Tetrabromotriazole
CASEIN KINASE II INHIBITOR I
4,5,6,7-TETRABROMOBENZOTRIAZOLE
CASEIN KINASE II INHIBITOR *TBB**
所屬類別
生物化工:激動劑抑制劑

物理化學性質(zhì)

熔點262-266°C
沸點552.5±45.0 °C(Predicted)
密度2.840±0.06 g/cm3(Predicted)
儲存條件2-8°C
儲存條件2-8°C
溶解度DMSO: 28 mg/mL
溶解度在DMSO中的溶解度為28 毫克/毫升
酸度系數(shù)(pKa)3.87±0.40(Predicted)
形態(tài)solid
顏色white
最大波長(λmax)300nm(MeOH)(lit.)

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險性描述H302-H315-H319-H335
WGK Germany3
WGK Germany3
海關編碼29349990

常見問題列表

生物活性
TBB是可滲透細胞,ATP競爭型的 CK2 抑制劑,抑制大鼠肝臟CK2的 IC50 值為0.15 μM。
靶點

CK2

0.15 μM (IC 50 , Human CK2)

PIM1

1.04 μM (IC 50 )

PIM2

4.3 μM (IC 50 )

PIM3

0.86 μM (IC 50 )

HIPK2

5.3 μM (IC 50 )

HIPK3

4.9 μM (IC 50 )

DYRK1a

4.36 μM (IC 50 )

DYRK2

0.99 μM (IC 50 )

DYRK3

5.3 μM (IC 50 )

PKD1

5.9 μM (IC 50 )

CDK2

14 μM (IC 50 )

體外研究

Investigation of the inhibitory power of TBB with a panel of 33 protein kinases shows highest potency for CK2 (casein kinase 2) (human CK2: IC 50 =1.6 μM at 100 μM ATP). TBB also inhibits three other kinases with less potency: CDK2 (IC 50 =15.6 μM), phosphorylase kinase (IC 50 =8.7 μM) and glycogen synthase kinase 3β (GSK3β) (IC 50 =11.2 μM). All other kinases tested have IC50 values 50-fold greater than that for CK2. The viability of the androgen insensitive PC-3 cells may be diminished by TBB (60 μM TBB) acting either alone or combined with anticancer agents CPT or TRAIL when a proper time schedule of the administration is applied. The time schedule-dependent activity of TBB does not come from its effect on apoptosis in PC-3 cells. TBB is an ATP/GTP competitive inhibitor of protein kinase casein kinase-2 (CK2), has been examined against a panel of 33 protein kinases, either Ser/Thr- or Tyr-specific. In the presence of 10 μM TBB (and 100 μM ATP) only CK2 is drastically inhibited (>85%) whereas three kinases (phosphorylase kinase, glycogen synthase kinase 3L and cyclin-dependent kinase 2/cyclin A) underwent moderate inhibition, with IC 50 values one-two orders of magnitude higher than CK2 (IC 50 =0.9 μM). TBB also inhibits endogenous CK2 in cultured Jurkat cells.

體內(nèi)研究

The extent of retinal neovascularization in a mouse OIR model is reduced by approximately 60% after treatment with TBB (6 days at 60 mg/kg per day).

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