Bisindolylmaleimide I HCl
Bisindolylmaleimide I HCl structure
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Common Name | Bisindolylmaleimide I HCl | ||
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| CAS Number | 176504-36-2 | Molecular Weight | 448.94500 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C25H25ClN4O2 | Melting Point | N/A | |
| MSDS | USA | Flash Point | N/A | |
Use of Bisindolylmaleimide I HClBisindolylmaleimide I (GF109203X) hydrochloride is a cell-permeable and reversible PKC inhibitor (IC50 of 20 nM, 17 nM, 16 nM, and 20 nM for PKCα, PKCβI, PKCβII, and PKCγ. Bisindolylmaleimide I hydrochloride is also a GSK-3 inhibitor[1][2][3]. |
| Name | 3-[1-[3-(dimethylamino)propyl]indol-3-yl]-4-(1H-indol-3-yl)pyrrole-2,5-dione,hydrochloride |
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| Synonym | More Synonyms |
| Description | Bisindolylmaleimide I (GF109203X) hydrochloride is a cell-permeable and reversible PKC inhibitor (IC50 of 20 nM, 17 nM, 16 nM, and 20 nM for PKCα, PKCβI, PKCβII, and PKCγ. Bisindolylmaleimide I hydrochloride is also a GSK-3 inhibitor[1][2][3]. |
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| Related Catalog | |
| Target |
Bovine brain PKC:10 nM (IC50) PKC-βII:16 nM (IC50) PKC-βI:17 nM (IC50) PKCα:20 nM (IC50) PKCγ:20 nM (IC50) FDGFG:65 μM (IC50) |
| In Vitro | Bisindolylmaleimide I hydrochloride (5 μM) 抑制 α-凝血酶诱导的 P47 磷酸化[1]。 Bisindolylmaleimide I hydrochloride (0-1 μM) 抑制静息态 swiss 3T3 细胞中的 DNA 合成[1]。 Bisindolylmaleimide I hydrochloride (5 μM) 可将脂肪细胞裂解物中的 GSK-3 活性降低至 25.1±4.3%[3]。 Bisindolylmaleimide I hydrochloride (10 μM，24 小时) 抑制 PC3 细胞释放外泌体和微泡 (EMV)[4]。 Bisindolylmaleimide I hydrochloride (10 μM，24 小时) 增强 5-fluorouracil (HY-90006) 的细胞毒性[4]。 |
| In Vivo | Bisindolylmaleimide I hydrochloride (0.02 mg/kg，腹腔注射.) 降低小鼠机械通气 (MV) 组中升高的 NLRP3、P-PKCɑ 和 PKCɑ 水平[5]。 Bisindolylmaleimide I hydrochloride (0-20 mg/kg，腹腔注射) 降低了鼩鼱中喹吡罗诱导的呕吐的平均频率[6]。 Animal Model: Quinpirole-treated shrews[2] Dosage: 0-20 mg/kg Administration: i.p. Result: Reduced the mean frequency of Quinpirole-induced vomiting. Blocked Quinpirole-mediated ERK1/2 phosphorylation in shrew brainstems. |
| References |
| Molecular Formula | C25H25ClN4O2 |
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| Molecular Weight | 448.94500 |
| Exact Mass | 448.16700 |
| PSA | 73.62000 |
| LogP | 4.71940 |
| Storage condition | -20℃ |
| Personal Protective Equipment | Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter |
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| RIDADR | NONH for all modes of transport |
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Protein kinase C-mediated phosphorylation of a single serine residue on the rat glial glutamine transporter SN1 governs its membrane trafficking.
J. Neurosci. 31 , 6565-75, (2011) Molecular mechanisms involved in the replenishment of the fast neurotransmitters glutamate and GABA are poorly understood. Glutamine sustains their generation. However, glutamine formation from the re... |
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The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C.
J. Biol. Chem. 266 , 15771, (1991) Staurosporine is the most potent inhibitor of protein kinase C (PKC) described in the literature with a half-maximal inhibitory concentration (IC50) of 10 nM. Nevertheless, this natural product is poo... |
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PDGF receptor activation induces p120-catenin phosphorylation at serine 879 via a PKCalpha-dependent pathway.
Exp. Cell Res. 315 , 39-49, (2009) p120-catenin (p120) is required for cadherin stability and is thought to have a central role in modulating cell-cell adhesion. Several lines of evidence suggest that S/T phosphorylation may regulate p... |
| Bisindolylmaleimide I,HCl |
| Bisindolylmaleimide I |
| 3-[1-(Dimethylaminopropyl)indol-3-yl]-4-(indol-3-yl)maleimide hydrochloride |
| Go-6850 |
| BIM I |
| Bisindolylmaleimide I hydrochloride |
| Bisindolylmaleimide |
| 2-[1-(3-Dimethylaminopropyl)-1H-indol-3-yl]-3-(1H-indol-3-yl)maleimide,HCl |