| Bioactivity | Bisindolylmaleimide I (GF109203X) 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 is also a GSK-3 inhibitor[1][2][3]. |
| Invitro | Bisindolylmaleimide I (5 μM) 抑制 α-凝血酶诱导的 P47 磷酸化[1]。Bisindolylmaleimide I (0-1 μM) 抑制静息态 swiss 3T3 细胞中的 DNA 合成[1]。Bisindolylmaleimide I (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 (10 μM，24 小时) 抑制 PC3 细胞释放外泌体和微泡 (EMV)[4]。Bisindolylmaleimide I (10 μM，24 小时) 增强 5-fluorouracil (HY-90006) 的细胞毒性[4]。 |
| In Vivo | Bisindolylmaleimide I (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 (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: |
| Name | Bisindolylmaleimide I |
| CAS | 133052-90-1 |
| Formula | C25H24N4O2 |
| Molar Mass | 412.48 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| Reference | [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. [3]. Hers I, et al. The protein kinase C inhibitors bisindolylmaleimide I (GF 109203x) and IX (Ro 31-8220) are potent inhibitors of glycogen synthase kinase-3 activity. FEBS Lett. 1999 Nov 5;460(3):433-6. [4]. Kosgodage US, et al. Chloramidine/Bisindolylmaleimide-I-Mediated Inhibition of Exosome and Microvesicle Release and Enhanced Efficacy of Cancer Chemotherapy. Int J Mol Sci. 2017 May 9;18(5):1007. [5]. Liu M, et al. Aerobic exercise alleviates ventilator-induced lung injury by inhibiting NLRP3 inflammasome activation. BMC Anesthesiol. 2022 Dec 1;22(1):369. [6]. Belkacemi L, et al. Signal transduction pathways involved in dopamine D2 receptor-evoked emesis in the least shrew (Cryptotis parva). Auton Neurosci. 2021 Jul;233:102807. |
Bisindolylmaleimide I
CAS: 133052-90-1 F: C25H24N4O2 W: 412.48
Bisindolylmaleimide I (GF109203X) is a cell-permeable and reversible PKC inhibitor (IC50 of 20 nM, 17 nM, 16 nM, and 20
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