Dorsomorphin (Compound C) (Synonyms: Compound C) |
カタログ番号GC17243
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Dorsomorphin (Compound C)はAMPKとBMP経路の強力で、細胞透過性を持つ二重阻害剤である（AMPKに対するKi値は109nM）。
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Cas No.: 866405-64-3
Sample solution is provided at 25 µL, 10mM.
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Dorsomorphin (Compound C)はAMPKとBMP経路の強力で、細胞透過性を持つ二重阻害剤である（AMPKに対するKi値は109nM）。Dorsomorphinは、AMPKのATP部位に競合的に結合し、AMPKの活性を阻害し、細胞エネルギー感知を遮断する。同時に、DorsomorphinはBMPのI型受容体ALK2/ALK3/ALK6を阻害し、SMAD1/5/8のリン酸化を遮断する。Dorsomorphinは、幹細胞の分化、腫瘍と代謝の研究に使える[1-4]。
In vitro（体外）実験で、Dorsomorphin（5μM）でJurkat、U937、Molt4、その他の急性リンパ芽球性白血病と急性骨髄性白血病細胞株を24時間処理した。Dorsomorphinは、細胞で、AMPKαの自己リン酸化、Beclin 1、Raptor、ULK1、ACCなどの下流AMPK基質のリン酸化を阻害した。Dorsomorphinはミトコンドリア経路細胞死を増強した[5]。Dorsomorphin（5μM）と分化誘発剤（0.5mMの3-isobutyl-1-methylxanthine、0.25μMのデキサメタゾン、10μg/mlのインスリン）を併用して3T3-L1前駆脂肪細胞を8日間処理した。Dorsomorphinは、3T3-L1前駆脂肪細胞で脂質の蓄積を著しく減らした[6]。
In vivo（体内）実験で、SAHモデリングの1時間後、くも膜下出血（SAH）モデルのCD-1雄マウスに、Dorsomorphin（10mg/kg；単回尾静脈注射）と組み換え型ヒトGPNMB（rGPNMB；単回脳室内注射）を投与した。Dorsomorphinは、マウスでp-AMPK/AMPK比を低下させた。Dorsomorphinは、rGPNMBによるp-NFκB、IL-1β、IL-6とTNF-αの下方制御を逆転させた。Dorsomorphinは、rGPNMB媒介の脳浮腫、血液脳関門の破壊、神経障害の軽減に対抗した[7]。各有酸素運動のセッションの1時間前に、Dorsomorphin（10mg/kg）を8週間APP/PS1マウスに腹腔内注射した。Dorsomorphinは、有酸素運動によるp300核転座の促進、海馬H4K5acとH4K12acの上方制御、GluN1プロモーター領域におけるヒストンアセチル化の濃縮を消した。Dorsomorphinは、有酸素運動により増強されたCA1樹状突起スパイン密度、LTPと文脈的恐怖記憶の改善に対抗した[8]。
| 細胞実験 [1]: | |
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細胞株 |
Jurkat、Molt4、CEM、REH、Nalm6（急性リンパ球白血病、ALL）、U937、THP.1、ML-1、HL-60、KG1A、MV-4-11、SET2（急性骨髄白血病、AML）、K562、HEL（慢性骨髄白血病の急性転化期）細胞株 |
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調製方法 |
10⁶個/mL以下の密度で、10%の加熱不活性化ウシ胎児血清（FBS）、100U/mLのペニシリンG、100μg/mLのストレプトマイシンと2mMのグルタミン酸を含有するRPMI 1640で上記の急性白血病細胞株を培養した。細胞をDorsomorphinで24時間処理した。 |
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反応条件 |
5μM；24時間 |
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応用 |
Dorsomorphinは細胞死を誘発した。Dorsomorphinは、AMPKαの自己リン酸化、下流AMPK基質（Beclin 1、Raptor、ULK1とACC）のリン酸化を抑制し、Ser75とSer99で、アポトーシス性タンパク質BADの脱リン酸化を促進し、ミトコンドリアへのBAD移行を促進し、BCLXLと結合させ、更にBAKの活性化、procaspase-9/procaspase-3/PARP1の切断を増やし、これにGSDME媒介のパイロトーシスは部分的に関与していた。 |
| 動物実験 [2]: | |
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動物モデル |
動脈穿刺により作製された雄CD-1 (ICR)マウス、くも膜下出血（SAH）モデル |
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調製方法 |
雄CD-1マウスを麻酔し、動脈穿刺を通じて、SAH誘発を行った。SAHモデリングが成功した1時間後、Dorsomorphinを尾静脈注射した。マウスを4つのグループに分けた：模擬手術、SAH+溶媒、SAH+組み換え型ヒトGPNMB（rGPNMB、3.3μg/10μL、SAHの1時間後に脳室内注射）とSAH+Dorsomorphin。 |
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剤形 |
10mg/kg；静脈内注射；SAHの1時間後、単回注射 |
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応用 |
DorsomorphinはSAHマウスで、rGPNMBにより上昇したp-AMPK/AMPKの比を低下させ、rGPNMBによるp-NFκB、IL-1β、IL-6とTNF-αの下方制御を逆転させ（タンパク質と分泌レベルの両方で）、脳浮腫、血液脳関門の破壊、神経学的な障害に対するrGPNMBの軽減作用に対抗した。 |
| Cas No. | 866405-64-3 | SDF | |
| 同義語 | Compound C | ||
| Chemical Name | 6-[4-(2-piperidin-1-ylethoxy)phenyl]-3-pyridin-4-ylpyrazolo[1,5-a]pyrimidine | ||
| Canonical SMILES | C1CCN(CC1)CCOC2=CC=C(C=C2)C3=CN4C(=C(C=N4)C5=CC=NC=C5)N=C3 | ||
| Formula | C24H25N5O | M.Wt | 399.49 |
| 溶解度 | 5mg/ml in DMSO with ultrasonic and warming | Storage | 4°C, protect from light |
| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5032 mL | 12.516 mL | 25.0319 mL |
| 5 mM | 500.6 μL | 2.5032 mL | 5.0064 mL |
| 10 mM | 250.3 μL | 1.2516 mL | 2.5032 mL |
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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- SDS (Safety Data Sheet)
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GCN2-IN-2 (A-92) (#GC32771-5) and Compound C (#GC17243) were obtained from GLPBIO.
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Dorsomorphin (10 μM) was purchased from Glpbio (California, USA).
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Selection and mechanism of the MTND therapy.(a) The cell morphology (bright field image) of tumor cells in its normal state (without any drug treatment); (b) tumor cell morphology (bright field image) under other drug combinations (Retinoic acid, Dorsomorphin, Purmorphamine,P7C3-A20);
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Related Biological Data
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