Bisindolylmaleimide IV (Synonyms: Arcyriarubin A,BIM IV) |
| Catalog No.GC14716 |
Bisindolylmaleimide IV는 IC50 값이 0.1-0.55μM인 효과적인 세포 투과성 단백질 산화효소 C (PKC) 저해제이다.
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Cas No.: 119139-23-0
Sample solution is provided at 25 µL, 10mM.
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Bisindolylmaleimide IV는 IC50 값이 0.1-0.55μM인 효과적인 세포 투과성 단백질 산화효소 C (PKC) 저해제이다. Bisindolylmaleimide IV는 cAMP 의존성 단백질 산화효소 (PKA)를 저해하는 IC50이 3.1-11.8μM 범위를 보인다[2]. Bisindolylmaleimide IV는 주로 암 생물학[3], 심혈관 질환[4] 그리고 당뇨병과 관련된 연구에서 사용되고 특히 PKC 매개 신호 경로와 그들이 세포 기능에 미치는 영향을 조사하는 연구에서 사용된다[5].
Bisindolylmaleimide IV(20μM)은 단핵구 유래 수목상세포에서 세포 시스테인 8(FLICE)-유사 저해 단백질(c-FLIPL)의 발현을 감소시키고 CD95 매개 사멸을 촉진한다[6]. Bisindolylmaleimide IV(0.1-100μM)은 IL-3, phorbol-12-myristate-13-acetate (PMA), 나트륨 플루오라이드 등에 의해 자극된 인간 중성구에서 생성되는 활성산소(ROS)의 방출을 용량 의존적으로 억제한다[7].
References:
[1]. Toullec D, Pianetti P, Coste H, 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. PMID: 1874734.
[2]. Fabre S, Prudhomme M, Rapp M. Protein kinase C inhibitors; structure-activity relationships in K252c-related compounds. Bioorg Med Chem. 1993 Sep;1(3):193-6. doi: 10.1016/s0968-0896(00)82121-5. PMID: 8081852.
[3]. Pajak B, Orzechowska S, Gajkowska B, Orzechowski A. Bisindolylmaleimides in anti-cancer therapy - more than PKC inhibitors. Adv Med Sci. 2008;53(1):21-31. doi: 10.2478/v10039-008-0028-6. PMID: 18635421.
[4]. Silnitsky S, Rubin SJS, Zerihun M, Qvit N. An Update on Protein Kinases as Therapeutic Targets-Part I: Protein Kinase C Activation and Its Role in Cancer and Cardiovascular Diseases. Int J Mol Sci. 2023 Dec 18;24(24):17600. doi: 10.3390/ijms242417600. PMID: 38139428; PMCID: PMC10743896.
[5].Anderson PW, McGill JB, Tuttle KR. Protein kinase C beta inhibition: the promise for treatment of diabetic nephropathy. Curr Opin Nephrol Hypertens. 2007 Sep;16(5):397-402. doi: 10.1097/MNH.0b013e3281ead025. PMID: 17693752.
[6]. Willems F, Amraoui Z, Vanderheyde N, et al. Expression of c-FLIP(L) and resistance to CD95-mediated apoptosis of monocyte-derived dendritic cells: inhibition by bisindolylmaleimide. Blood. 2000 Jun 1;95(11):3478-82. PMID: 10828032.
[7]. Krämer HJ, Kessler D, Hipler UC, et al. Pityriarubins, novel highly selective inhibitors of respiratory burst from cultures of the yeast Malassezia furfur: comparison with the bisindolylmaleimide arcyriarubin A. Chembiochem. 2005 Dec;6(12):2290-7. doi: 10.1002/cbic.200500163. PMID: 16252297.
| 세포 실험 [1]: | |
세포 라인 | 수지상 세포 |
제조 방법 | 수목상세포는 항-CD95 단일클론항체(0.5μg/mL)가 있는 배양액에서 Bisindolylmaleimide IV(20μM)와 함께 또는 함께하지 않고 배양되었습니다. 18시간 후 세포는 고정되었고 DNA는 프로피디움 아이오디드(PI)로 염색되었고 하이포디프로그래믹 핵(subG1 peak)의 비율은 유세포 분석기로 분석되었습니다. |
반응 조건 | 20μM; 18시간 동안 |
응용 분야 | Bisindolylmaleimide IV는 항-CD95 mAb에 의해 유도된 세포사멸을 촉진합니다. |
References: | |
| Cas No. | 119139-23-0 | SDF | |
| Synonyms | Arcyriarubin A,BIM IV | ||
| Chemical Name | 3,4-di-1H-indol-3-yl-1H-pyrrole-2,5-dione | ||
| Canonical SMILES | O=C1NC(=O)C(=C1c1c[nH]c2ccccc12)c1c[nH]c2ccccc12 | ||
| Formula | C20H13N3O2 | M.Wt | 327.3 |
| Solubility | ≤20mg/ml in ethanol;20mg/ml in DMSO;20mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.0553 mL | 15.2765 mL | 30.553 mL |
| 5 mM | 0.6111 mL | 3.0553 mL | 6.1106 mL |
| 10 mM | 0.3055 mL | 1.5277 mL | 3.0553 mL |
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Quality Control & SDS
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- Purity: >97.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 3 reference(s) in Google Scholar.)
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