Art. -Nr.: HY-13495

ML281

2 Cited Publications

Kundenbewertung

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

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Reinheit: 98.04%
CAS. Nr.: 1404437-62-2
Formel: C₂₂H₁₉N₃O₂S
Molecular Weight:389.47

Speicherung:

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

ML281 Chemical Structure

CAS. Nr.: 1404437-62-2

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Publications (2)
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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

Alle PKA Isoform-spezifische Produkte anzeigen :

Alle Aurora Kinase Isoform-spezifische Produkte anzeigen :

Alle Bcl-2 Family Isoform-spezifische Produkte anzeigen :

In Vitro

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.

Chemical Information

CAS. Nr. 1404437-62-2
Appearance Solid
Molecular Weight 389.47
Formel C₂₂H₁₉N₃O₂S
Color White to off-white
SMILES

O=C1NC2=CC=CC=C2N=C1C3=CC(C(C)C)=CC=C3NC(C4=CC=CS4)=O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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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Journal Impact Factor

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.

Lösungsmittel & Löslichkeit

In Vitro:

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (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)
Elemental Analysis Report (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)
Handling Instructions (2659 KB)

Verweise

[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

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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

Publications Citing Use of MedChemExpress (MCE) ML281

Alle PKA Isoform-spezifische Produkte anzeigen

Alle Aurora Kinase Isoform-spezifische Produkte anzeigen

Alle Bcl-2 Family Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

ML281 Related Classifications

HY-13495 Related Classifications