Bisindolylmaleimide II is a general inhibitor of all PKC subtypes[1].
分子量
438.52
Formula
C27H26N4O2
CAS 号
137592-45-1
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Gassel M, et al. The protein kinase C inhibitor bisindolyl maleimide 2 binds with reversed orientations to different conformations of protein kinase A. J Biol Chem. 2004 May 28;279(22):23679-90.
Bisindolylmaleimide II is a general inhibitor of all PKC subtypes[1].
分子量
438.52
Formula
C27H26N4O2
CAS 号
137592-45-1
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Gassel M, et al. The protein kinase C inhibitor bisindolyl maleimide 2 binds with reversed orientations to different conformations of protein kinase A. J Biol Chem. 2004 May 28;279(22):23679-90.
Bisindolylmaleimide II is a general inhibitor of all PKC subtypes[1].
分子量
438.52
Formula
C27H26N4O2
CAS 号
137592-45-1
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Gassel M, et al. The protein kinase C inhibitor bisindolyl maleimide 2 binds with reversed orientations to different conformations of protein kinase A. J Biol Chem. 2004 May 28;279(22):23679-90.
Bisindolylmaleimide I(Synonyms: GF109203X; Go 6850) 纯度: 99.03%
Bisindolylmaleimide I (GF109203X) 是一种高度选择,可渗透细胞,可逆的 PKC抑制剂,Ki 值为14 nM。
Bisindolylmaleimide I Chemical Structure
CAS No. : 133052-90-1
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生物活性
Bisindolylmaleimide I (GF109203X) is a highly selective, cell-permeable, and reversible protein kinase C (PKC) inhibitor with a Ki of 14 nM.
IC50 & Target
Bovine brain PKC
10 nM (IC50)
PKCβII
16 nM (IC50)
PKCβI
17 nM (IC50)
PKCα
20 nM (IC50)
PKCγ
20 nM (IC50)
FDGFR
65 μM (IC50)
体外研究 (In Vitro)
Bisindolylmaleimide I is a competitive inhibitor with respect to ATP (Ki=14 nM) and displays high selectivity for PKC as compared to five different protein kinases. GF 109203X efficiently prevents PKC-mediated phosphorylations of an Mr=47,000 protein in platelets and of an Mr=80,000 protein in Swiss 3T3 cells. GF 109203X inhibits collagen- and a-thrombin-induced platelet aggregation as well as collagen-triggered ATP secretion. However, ADP-dependent reversible aggregation is not modified. In Swiss 3T3 fibroblasts, GF 109203X reverses the inhibition of epidermal growth factor binding induced by phorbol 12,13-dibutyrate and prevents [3H] thymidine incorporation into DNA, only when this is elicited by growth promoting agents which activate PKC[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
Pial arteriole diameter changes are monitored using a closed cranial window in vivo microscopy technique. The pial arteriole dilatory response associated with SNS is decreased by 45%, when comparing DM vs either ND or TR rats. Also, pial arteriolar dilations to topical KCl and NS1619 are largely attenuated in DM rats, but not in ND or TR animals. These responses are completely restored by the acute application of Bisindolylmaleimide I to the brain surface. The PKC inhibitor has no effect on vascular responses in normoglycemic and TR animals. In conclusion, DM-associated chronic impairment of neurovascular coupling may be readily reversed by a PKC-α/β/γ inhibitor or prevented via pancreatic islet transplantation. Specific PCK isoforms (α/β/γ) are believed to be mechanistically linked to the neurovascular uncoupling seen with hyperglycemia[2].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
412.48
Formula
C25H24N4O2
CAS 号
133052-90-1
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Toullec D, et al. The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C. J Biol Chem. 1991 Aug 25;266(24):15771-81.
[2]. Vetri F, et al. Impairment of neurovascular coupling in Type 1 Diabetes Mellitus in rats is prevented by pancreatic islet transplantation and reversed by a semi-selective PKC inhibitor. Brain Res. 2017 Jan 15;1655:48-54.
Kinase Assay [1]
Assay of PKC is arrayed by measuring 32Pi transferred from [γ-32Pi] ATP to lysine-rich histone type Ill-s. The reaction mixture (80 μL) contains 50 mM Tris-HCI, pH 7.4. 100 μM CaCl2, 10 mM MgCI2, 37.5 μg/mL histone type Ill-s, l0 μM [γ-32Pi] ATP (1250cpm/pmol), 31 μM bovine brain phosphatidylserine and 0.5 μM 1,2 sn-dioleylglycerol. 15 μL of purified PKC (final concentration in assay 0.38 μg/mL) is added to the incubation mixture. After 10 minutes, the reaction is stopped by addition of at 30 μL of casein 30 mg/mL and 0.9 mL of 12% trichlomacetic acid[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration [2]
Three sets of Lewis rats is used for this study: 1) euglycemic 4–6 month old non-diabetic controls (ND group, n=11); 2) streptozotocin (STZ)-treated diabetic rats (6 month old, 4 months post-STZ) (DM group, n=6); and 3) STZ-treated diabetic animals, subjected to pancreatic islet transplantation soon after the establishment of the diabetic model, studied 100–110 days after the transplant (TR group, n=7)[2].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献
[1]. Toullec D, et al. The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C. J Biol Chem. 1991 Aug 25;266(24):15771-81.
[2]. Vetri F, et al. Impairment of neurovascular coupling in Type 1 Diabetes Mellitus in rats is prevented by pancreatic islet transplantation and reversed by a semi-selective PKC inhibitor. Brain Res. 2017 Jan 15;1655:48-54.