製品番号: HY-13495

ML281

2 Cited Publications

カスタマーレビュー

Based on 2 publication(s) in Google Scholar

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

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

純度: 98.04%
CAS 番号: 1404437-62-2
分子式: C₂₂H₁₉N₃O₂S
分子量:389.47

保管条件:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

ML281 構造式

CAS 番号: 1404437-62-2

容量

価格（税別）

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数量

Amount: USD 0.00

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性

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

PKA アイソフォーム固有の製品をすべて表示 :

Aurora Kinase アイソフォーム固有の製品をすべて表示 :

Bcl-2 Family アイソフォーム固有の製品をすべて表示 :

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.

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.

化学情報

CAS 番号 1404437-62-2
性状 Solid
分子量 389.47
分子式 C₂₂H₁₉N₃O₂S
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	2 years
	-20°C	1 year

Publications (2)

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Nat Commun

HPD degradation regulated by the TTC36-STK33-PELI1 signaling axis induces tyrosinemia and neurological damage. [Abstract]

2019 Sep 19;10(1):4266. PMID: 31537781
Neoplasma

Knockdown of human serine/threonine kinase 33 suppresses human small cell lung carcinoma by blocking RPS6/BAD signaling transduction. [Abstract]

2017;64(6):869-879. PMID: 28895411

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.

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

モル濃度計算機

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (285 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[1]. Sun EL, et al. Knockdown of human serine/threonine kinase 33 suppresses human small cell lung carcinoma by blocking RPS6/BAD signaling transduction. Neoplasma. 2017;64(6):869-879.

[2]. Weïwer M, et al. A Potent and Selective Quinoxalinone-Based STK33 Inhibitor Does Not Show Synthetic Lethality in KRAS-Dependent Cells. ACS Med Chem Lett. 2012 Dec 13;3(12):1034-1038.

[3]. Spoonamore J et al. Screen for Inhibitors of STK33 Kinase Activity. National Center for Biotechnology Information (US); 2010-2011 Dec 16. [Content Brief]

[4]. Xie Y, et al. HPD degradation regulated by the TTC36-STK33-PELI1 signaling axis induces tyrosinemia and neurological damage. Nat Commun. 2019 Sep 19;10(1):4266.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

ML281

2 Cited Publications

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ML281

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Kinase Inhibitor Library

Stem Cell Signaling Compound Library

TGF-beta/Smad Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Mitochondria-Targeted Compound Library

Targeted Diversity Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Heterocyclic Compound Library

Pain-Related Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Mitophagy Compound Library

Bioactive Compound Library Max

Kinase Inhibitor Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

MedChemExpress（MCE）の使用を引用している文献 ML281

PKA アイソフォーム固有の製品をすべて表示

Aurora Kinase アイソフォーム固有の製品をすべて表示

Bcl-2 Family アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (2)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

ML281 関連分類

HY-13495 関連分類