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Product Name:Bisindolylmaleimide I hydrochloride
CAS:176504-36-2
Purity:>=98% Remarks:Reach out to us for more information about custom solutions.
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| Company Name: |
Bide Pharmatech Ltd.
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400-400-164-7117 18317119277 |
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Product Name:3-(1-(3-(Dimethylamino)propyl)-1H-indol-3-yl)-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione hydrochloride
CAS:176504-36-2
Purity:98% Package:5mg;10mg;25mg;50mg Remarks:BD01108358
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| | BISINDOLYLMALEIMIDE I HYDROCHLORIDE Basic information |
| Product Name: | BISINDOLYLMALEIMIDE I HYDROCHLORIDE | | Synonyms: | BIM 1 hydrochloride;3-[1-(dimethylaminopropyl)indol-3-yl]-4-(indol-3-yl)maleimide hydrochloride;BisindolylMaleiMide I( Hydrochloride Salt);BisindolylMaleiMide I . hydrochloride [GF-109203K;3-[1-[3-(Dimethylamino)propyl]-1H-indol-3-yl]-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione monohydrochloride;3-[1-[3-(dimethylamino)propyl]indol-3-yl]-4-(1H-indol-3-yl)pyrrole-2,5-dione;Bisindolylmaleimide I, Hydrochloride - CAS 176504-36-2 - Calbiochem;GF 109203X hydrochloride >=95% | | CAS: | 176504-36-2 | | MF: | C25H25ClN4O2 | | MW: | 448.95 | | EINECS: | | | Product Categories: | | | Mol File: | 176504-36-2.mol |  |
| | BISINDOLYLMALEIMIDE I HYDROCHLORIDE Chemical Properties |
| storage temp. | 2-8°C | | solubility | DMF: 10 mg/mL; DMSO: 16 mg/mL; DMSO:PBS(pH 7.2) (1:4): 0.2 mg/mL | | form | Orange-red solid | | color | Orange to red | | biological source | synthetic (organic) | | Water Solubility | water: 10mg/mL
DMSO: 20mg/mL | | InChIKey | XRAMWNCMYJHGGH-UHFFFAOYSA-N | | SMILES | Cl.CN(C)CCCn1cc(C2=C(C(=O)NC2=O)c3c[nH]c4ccccc34)c5ccccc15 |
| WGK Germany | 3 | | HS Code | 2933998090 | | Storage Class | 11 - Combustible Solids |
| | BISINDOLYLMALEIMIDE I HYDROCHLORIDE Usage And Synthesis |
| Description | Bisindolylmaleimide I (BIM I) is a highly selective, cell-permeable, and reversible PKC inhibitor (Ki = 14 nM) that is structurally similar to the poorly selective PKC inhibitor staurosporine . It acts as a competitive inhibitor for the ATP binding site of PKC and shows high selectivity for PKCα, β1, β2, γ, δ, and ε isozymes. BIM I directly inhibits glycogen synthase kinase 3 (GSK3) in primary adipocyte lysates (IC50 = 360 nM) and in GSK3β immunoprecipitates derived from rat epididymal adipocytes (IC50 = 170 nM). It also competitively antagonizes the serotonin (5-HT) receptor subtype 5-HT3 with a Ki value of 61 nM. | | Uses | GF 109203X hydrochloride has been used to inhibit protein kinase C in human neuroblastoma-derived kelly cells. | | General Description | GF 109203X prevents collagen-triggered adenosine and three phosphate (ATP) secretion. It also inhibits collagen and α-thrombin-induced platelet aggregation. It functions as an inhibitor of glycogen synthase kinase-3 (GSK-3). GF 109203X also functions as an anti-inflammatory agent. | | Biochem/physiol Actions | Inhibitor of protein kinase C; potent inhibitor of GSK-3. | | in vivo | Bisindolylmaleimide I hydrochloride (0.02 mg/kg, i.p.) reduced the inceased NLRP3, P-PKCɑ, and PKCɑ levels in mechanical ventilation (MV) group[5].
Bisindolylmaleimide I hydrochloride (0-20 mg/kg, i.p.) reduces the mean frequency of Quinpirole-induced vomiting in shrews[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.
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| | IC 50 | 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) | | References | [1] D. TOULLEC. The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C.[J]. The Journal of Biological Chemistry, 1991, 12 1: 15771-15781. DOI: 10.1016/s0021-9258(18)98476-0
[2] INGEBORG HERS Richard M D Jeremy M Tavaré. The protein kinase C inhibitors bisindolylmaleimide I (GF 109203x) and IX (Ro 31-8220) are potent inhibitors of glycogen synthase kinase-3 activity[J]. FEBS Letters, 1999, 460 3: 433-436. DOI: 10.1016/s0014-5793(99)01389-7
[3] S J COULTRAP. Competitive antagonism of the mouse 5-hydroxytryptamine3 receptor by bisindolylmaleimide I, a “selective” protein kinase C inhibitor.[J]. Journal of Pharmacology and Experimental Therapeutics, 1999, 290 1: 76-82.
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| | BISINDOLYLMALEIMIDE I HYDROCHLORIDE Preparation Products And Raw materials |
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