2. Cell Cycle/DNA Damage TGF-beta/Smad Stem Cell/Wnt Epigenetics Apoptosis
  3. STK33 PKA Aurora Kinase Bcl-2 Family Apoptosis
  4. ML281

ML281 is a highly selective inhibitor of serine/threonine kinase 33 (STK33) with an IC50 value of 14 nM. ML281 shows 700-fold selectivity over PKA and 550-fold over AurB. ML281 exerts core mechanism by inhibiting STK33: in small cell lung cancer, ML281 downregulates RPS6/BAD signaling phosphorylation, induces apoptosis, and suppresses proliferation, invasion. ML281 reduces STK33-mediated 4-hydroxyphenylpyruvate dioxygenase (HPD) phosphorylation in tyrosinemia . ML281 is suitable for research on STK33 function, KRAS mutation-related cancers (pancreatic cancer, colon cancer, lung adenocarcinoma, etc.), small cell lung cancer, and tyrosinemia-related damage

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CAS 番号 : 1404437-62-2

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10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 99 在庫あり
Solid
5 mg $90 在庫あり
10 mg $126 在庫あり
25 mg $250 在庫あり
50 mg $400 在庫あり
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Based on 2 publication(s) in Google Scholar

ML281 関連抗体

Top Publications Citing Use of Products

    ML281 purchased from MedChemExpress. Usage Cited in: Neoplasma. 2017;64(6):869-879.  [Abstract]

    Representative images and analysis results of western blotting validation after incubation with ML281.

    PKA アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    PKA PKAR PKACα

    Aurora Kinase アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    Aurora Kinase Aurora A Aurora B Aurora C

    Bcl-2 Family アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

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    製品説明

    ML281 is a highly selective inhibitor of serine/threonine kinase 33 (STK33) with an IC50 value of 14 nM. ML281 shows 700-fold selectivity over PKA and 550-fold over AurB. ML281 exerts core mechanism by inhibiting STK33: in small cell lung cancer, ML281 downregulates RPS6/BAD signaling phosphorylation, induces apoptosis, and suppresses proliferation, invasion[1]. ML281 reduces STK33-mediated 4-hydroxyphenylpyruvate dioxygenase (HPD) phosphorylation in tyrosinemia [4]. ML281 is suitable for research on STK33 function, KRAS mutation-related cancers (pancreatic cancer, colon cancer, lung adenocarcinoma, etc.), small cell lung cancer, and tyrosinemia-related damage[1][2][4]

    IC50 & Target[1]

    PKA

     

    Aurora B

     

    bad

     

    体外実験

    ML281 (10 μM; 72 hours) suppresses cell viability of NCI-H446 cells[3].
    ML281 exhibits potent inhibitory activity against purified recombinant serine/threonine kinase 33 (STK33) (IC50 = 14 nM) [1].
    ML281 (0.01-10 μM) has no significant effect on the viability of KRAS-dependent (NOMO-1, SKM-1) and KRAS-independent (THP-1, U937) acute myeloid leukemia-derived cell lines, ML281 does not exhibit selective cytotoxicity against KRAS-dependent cancer cells.[1].
    ML281 (10 μM; 72 h) suppresses RPS6/BAD signaling pathway in human small cell lung cancer NCI-H446 cells[1].
    ML281 (2.5-12.5 μM; 48 h) decreases T382 site phosphorylation of 4-hydroxyphenylpyruvate dioxygenase (HPD) and increases HPD protein expression in a dosage-dependent manner in human fetal hepatocyte LO2 cells[4].
    ML281 (10 μM; 48 h) abrogates enhanced HPD T382 phosphorylation and HPD degradation in Ttc36-deficient mouse primary hepatocytes[4].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    ML281 関連抗体

    Cell Viability Assay[3]

    Cell Line: NCI-H446 cells
    Concentration: 10 μM
    Incubation Time: 72 hours
    Result: Suppressed cell viability of NCI-H446 cells.

    Western Blot Analysis[4]

    Cell Line: LO2 cells
    Concentration: 2.5 μM, 5 μM, 7.5 μM, 10 μM, 12.5 μM
    Incubation Time: 48 h
    Result: Decreased HPD T382 phosphorylation, increased HPD protein expression in a dosage-dependent manner; no effect on HPD T382A mutant phosphorylation.

    Western Blot Analysis[4]

    Cell Line: Ttc36-/- mouse primary hepatocytes
    Concentration: 10 μM
    Incubation Time: 48 h
    Result: Abrogated enhanced HPD T382 phosphorylation and HPD degradation induced by TTC36 deficiency.

    Western Blot Analysis[3]

    Cell Line: NCI-H446 cells
    Concentration: 10 μM
    Incubation Time: 72 hours
    Result: Decreased phosphorylation of RPS6 and BAD, increased expression of cleaved caspase 9.
    分子量

    389.47

    分子式

    C22H19N3O2S
    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C1NC2=CC=CC=C2N=C1C3=CC(C(C)C)=CC=C3NC(C4=CC=CS4)=O
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : 100 mg/mL (256.76 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.5676 mL 12.8380 mL 25.6759 mL
    5 mM 0.5135 mL 2.5676 mL 5.1352 mL
    10 mM 0.2568 mL 1.2838 mL 2.5676 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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    参考文献

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.5676 mL 12.8380 mL 25.6759 mL 64.1898 mL
    5 mM 0.5135 mL 2.5676 mL 5.1352 mL 12.8380 mL
    10 mM 0.2568 mL 1.2838 mL 2.5676 mL 6.4190 mL
    15 mM 0.1712 mL 0.8559 mL 1.7117 mL 4.2793 mL
    20 mM 0.1284 mL 0.6419 mL 1.2838 mL 3.2095 mL
    25 mM 0.1027 mL 0.5135 mL 1.0270 mL 2.5676 mL
    30 mM 0.0856 mL 0.4279 mL 0.8559 mL 2.1397 mL
    40 mM 0.0642 mL 0.3209 mL 0.6419 mL 1.6047 mL
    50 mM 0.0514 mL 0.2568 mL 0.5135 mL 1.2838 mL
    60 mM 0.0428 mL 0.2140 mL 0.4279 mL 1.0698 mL
    80 mM 0.0321 mL 0.1605 mL 0.3209 mL 0.8024 mL
    100 mM 0.0257 mL 0.1284 mL 0.2568 mL 0.6419 mL
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    ML281 Related Classifications

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    ML2811404437-62-2ML 281ML-281STK33PKAAurora KinaseBcl-2 FamilyApoptosisSerine/threonine kinase 33Protein kinase ASTK33 inhibitorNCI-H446 cellsDMS153 cellsLO2 cellsNOMO-1 cellsSKM-1 cellsTHP-1 cellsU937 cellsBALB/c-nu micesmall cell lung cancer (SCLC)tyrosinemia type IIIKRAS-mutant cancerspancreatic cancercolon cancerlung adenocarcinomaneurological damagedownregulated RPS6/BAD signaling pathwaystabilize 4-hydroxyphenylpyruvate dioxygenase (HPD) expressionapoptosissuppressed tumor cell proliferationinhibited tumor cell invasionsuppressed xenograft tumor growthInhibitorinhibitorinhibit

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    製品名:
    ML281
    製品番号:
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