Art. -Nr.: HY-101494

Temuterkib

(Synonyms: LY3214996)

35 Cited Publications

Kundenbewertung

Based on 35 publication(s) in Google Scholar

Temuterkib (LY3214996) is a highly selective inhibitor of ERK1 and ERK2, with IC₅₀ of 5 nM for both enzymes in biochemical assays. Temuterkib potently inhibits cellular p-RSK1 in BRAF and RAS mutant cancer cell lines. Temuterkib shows potent antitumor activities in cancer models with MAPK pathway alterations.

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Reinheit: 99.93%
CAS. Nr.: 1951483-29-6
Formel: C₂₂H₂₇N₇O₂S
Molecular Weight:453.56

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Temuterkib Chemical Structure

CAS. Nr.: 1951483-29-6

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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
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (35)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

ERK1

5 nM (IC₅₀)

ERK2

5 nM (IC₅₀)

Alle ERK Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
SK-MEL-2	IC₅₀	1 μM Compound: LY3214996	Synergistic cytotoxicity against human SK-MEL-2 cells expressing NRAS mutant assessed as cell growth inhibition measured for 48 hrs in presence of MK2206 by MTT assay Synergistic cytotoxicity against human SK-MEL-2 cells expressing NRAS mutant assessed as cell growth inhibition measured for 48 hrs in presence of MK2206 by MTT assay	[PMID: 36961300]
SK-MEL-2	IC₅₀	1 μM Compound: LY3214996	Synergistic cytotoxicity against human SK-MEL-2 cells expressing NRAS mutant assessed as cell growth inhibition measured for 48 hrs in presence of Rapamycin by MTT assay Synergistic cytotoxicity against human SK-MEL-2 cells expressing NRAS mutant assessed as cell growth inhibition measured for 48 hrs in presence of Rapamycin by MTT assay	[PMID: 36961300]

In Vitro

Temuterkib is a highly selective inhibitor of ERK1 and ERK2, with IC₅₀ of 5 nM for both enzymes in biochemical assays. Temuterkib potently inhibits cellular phospho-RSK1 in BRAF and RAS mutant cancer cell lines. In an unbiased tumor cell panel sensitivity profiling for inhibition of cell proliferation, tumor cells with MAPK pathway alterations including BRAF, NRAS or KRAS mutation are generally sensitivity to Temuterkib^[1].

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

In Vivo

In tumor xenograft models, Temuterkib inhibits PD biomarker phospho-p90RSK1 in tumors and the PD effects are correlated with compound exposures and anti-tumor activities. Temuterkib shows either similar or superior anti-tumor activity as compared to other published ERK inhibitors in BRAF or RAS mutant cell lines and xenograft models. Oral administration of single-agent Temuterkib significantly inhibits tumor growth in vivo and is well tolerated in BRAF or NRAS mutant melanoma, BRAF or KRAS mutant colorectal, lung and pancreatic cancer xenografts or PDX models. Therefore, Temuterkib can be tailored for treatment of cancers with MAPK pathway alteration. In addition, Temuterkib has anti-tumor activity in a PLX4032-resistant A375 melanoma xenograft model due to MAPK reactivation, may have potential for treatment of melanoma patients who have failed BRAF therapies. More importantly, Temuterkib can be combined with investigational and approved agents in preclinical models, particularly KRAS mutant models. Combination treatment of Temuterkib and CDK4/6 inhibitor abemaciclib is well tolerated and results in potent tumor growth inhibition or regression in multiple in vivo cancer models, including KRAS mutant colorectal and non-small cell lung cancers^[1].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1951483-29-6
Appearance Solid
Molecular Weight 453.56
Formel C₂₂H₂₇N₇O₂S
Color White to yellow
SMILES

O=C(C(C=C(C1=NC(NC2=CC=NN2C)=NC=C1)S3)=C3C4(C)C)N4CCN5CCOCC5
Synonyms

LY3214996
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (35)

All IPWBBio/Physico-chemical AssayIF

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Journal Impact Factor

Signal Transduct Target Ther

The cross-talk between methylation and phosphorylation in lymphoid-specific helicase drives cancer stem-like properties. [Abstract]

2020 Sep 30;5(1):197. PMID: 32994405

Temuterkib purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2020 Sep 30;5(1):197. [Abstract]

Endogenous and exogenous LSH were respectively immunoprecipitated from A549 and 293T cells after treatment with the MAPK1/2 inhibitor Temuterkib for the indicated time, and then IB assay was carried out to detect the phosphorylated LSH with anti-phosphoserine antibody.

Temuterkib purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2020 Sep 30;5(1):197. [Abstract]

IP followed by IB assay in PC9 cell lines stably expressing LSH after treatment with the MAPK1/2 inhibitor Temuterkib for the indicated time.
Immunity

Modulation of the mevalonate pathway by TCR engagement regulates T follicular helper cell generation in homeostasis and autoimmunity. [Abstract]

2026 May 13:S1074-7613(26)00171-8. PMID: 42134327
Autophagy

USP13 facilitates a ferroptosis-to-autophagy switch by activation of the NFE2L2/NRF2-SQSTM1/p62-KEAP1 axis dependent on the KRAS signaling pathway. [Abstract]

2025 Mar;21(3):565-582. PMID: 39360581

Temuterkib purchased from MedChemExpress. Usage Cited in: Autophagy. 2025 Mar;21(3):565-582. [Abstract]

Western blot analysis of sgCtrl, sgUSP13^#1 or sgUSP13^#2 A549 cell lysates treated with DMSO or Temuterkib (LY3214996, 10 μM, 24 h) and probed with the indicated antibodies.
Mol Cell

OTUB2 Promotes Cancer Metastasis via Hippo-Independent Activation of YAP and TAZ. [Abstract]

2019 Jan 3;73(1):7-21.e7. PMID: 30472188
Theranostics

FGF19/SOCE/NFATc2 signaling circuit facilitates the self-renewal of liver cancer stem cells. [Abstract]

2021 Mar 5;11(10):5045-5060. PMID: 33754043

Temuterkib purchased from MedChemExpress. Usage Cited in: Theranostics. 2021 Mar 5;11(10):5045-5060. [Abstract]

Cells were pre-treated with DMSO, 3-NC (20 µM), Temuterkib (LY3214996, 2 µM), or 3-NC (20 µM) + Temuterkib (LY3214996, 2 µM) for 2h, respectively; then Ca²⁺ mobilization in Fura-2-loaded cells respectively upon FGF19 stimulation were measured and expressed as means ± SEM of 12 independent cells each group.

Temuterkib purchased from MedChemExpress. Usage Cited in: Theranostics. 2021 Mar 5;11(10):5045-5060. [Abstract]

Subcellular location of NFATc2 after FGF19 treatment: Huh-7 NCSCs were pre-treated with DMSO, BLU9931 (100 nM), 3-NC (20 µM), Temuterkib (LY3214996, 2 µM), 3-NC (20 µM) + Temuterkib (LY3214996, 2 µM), SKF96365 (5 µM), and FK506 (50 nM) for 2h, respectively; then treated with FGF19 (100 ng/ml) for 4h.

Temuterkib purchased from MedChemExpress. Usage Cited in: Theranostics. 2021 Mar 5;11(10):5045-5060. [Abstract]

Subcellular location of NFATc2 after FGF19 treatment: Huh-7 NCSCs were pre-treated with DMSO, BLU9931 (100 nM), 3-NC (20 µM), Temuterkib (LY3214996, 2 µM), 3-NC (20 µM) + Temuterkib (LY3214996, 2 µM), SKF96365 (5 µM), and FK506 (50 nM) for 2h, respectively; then treated with FGF19 (100 ng/ml) for 4h.
Cell Rep Med

Targeting the noncanonical function of metabolic enzyme PHGDH in driving PD-L1 expression and cancer immune evasion. [Abstract]

2026 Mar 26:102704. PMID: 41905348
Cell Death Dis

4EBP1 senses extracellular glucose deprivation and initiates cell death signaling in lung cancer. [Abstract]

2022 Dec 27;13(12):1075. PMID: 36575176
Phytomedicine

Unveiling poliumoside: A herbal-derived FAK kinase inhibitor with anti-proliferative and anti-metastatic efficacy. [Abstract]

2025 Dec 30:150:157747. PMID: 41485292
Diabetes

Chronic Glucocorticoid Exposure Induced a S1PR2-RORγ Axis to Enhance Hepatic Gluconeogenesis in Male Mice. [Abstract]

2023 Nov 1;72(11):1534-1546. PMID: 37552863
Mol Med

Activation of the MEK1-CHK2 axis in macrophages by Staphylococcus aureus promotes mitophagy, resulting in a reduction in bactericidal efficacy. [Abstract]

2025 May 29;31(1):211. PMID: 40437411
EMBO Mol Med

Thioparib inhibits homologous recombination repair, activates the type I IFN response, and overcomes olaparib resistance. [Abstract]

2023 Mar 8;15(3):e16235. PMID: 36652375
Stem Cell Res Ther

SMYD1 modulates the proliferation of multipotent cardiac progenitor cells derived from human pluripotent stem cells during myocardial differentiation through GSK3β/β-catenin&ERK signaling. [Abstract]

2024 Oct 8;15(1):350. PMID: 39380045
Cell Rep

Liver-derived plasminogen mediates muscle stem cell expansion during caloric restriction through the plasminogen receptor Plg-RKT. [Abstract]

2024 Mar 4;43(3):113881. PMID: 38442019
J Med Chem

Platinum-Paeonol Complexes as ERK Inhibitors To Restrain Melanoma and Relieve Cancer Pain. [Abstract]

2026 Apr 9;69(7):7663-7676. PMID: 41873204
Front Immunol

IL-27 Mediates Pro-Inflammatory Effects via the ERK Signaling Pathway During Preterm Labor. [Abstract]

2021 Oct 8;12:709229. PMID: 34691022
Biochem Pharmacol

Glimepiride overcomes acquired resistance to EGFR TKIs in lung cancer via the AMPK/ERK/MMP7 signaling pathway. [Abstract]

2025 Jul 12:241:117162. PMID: 40659128
Cancer Biol Ther

Repeated treatments of Capan-1 cells with PARP1 and Chk1 inhibitors promote drug resistance, migration and invasion. [Abstract]

2022 Dec 31;23(1):69-82. PMID: 35000525
Respir Res

CREB-dependent LPA-induced signaling initiates a pro-fibrotic feedback loop between small airway basal cells and fibroblasts. [Abstract]

2021 Apr 1;22(1):97. PMID: 33794877
Cancer Sci

Antitumor activity of Raddeanin A is mediated by Jun amino-terminal kinase activation and signal transducer and activator of transcription 3 inhibition in human osteosarcoma. [Abstract]

2019 May;110(5):1746-1759. PMID: 30907478

Temuterkib purchased from MedChemExpress. Usage Cited in: Cancer Sci. 2019 May;110(5):1746-1759. [Abstract]

Cells are treated with RA in the presence or absence of the Erk1/2 inhibitor LY3214996, phospho-Erk1/2, Erk1/2, phospho-JNK, JNK, phospho-c-Jun, c-Jun, total and cleaved PARP, phospho-STAT3S727, and STAT3 are analyzed.
Neoplasia

STAMBP promotes lung adenocarcinoma metastasis by regulating the EGFR/MAPK signaling pathway. [Abstract]

2021 Jun;23(6):607-623. PMID: 34102455
iScience

A defective mechanosensing pathway affects fibroblast-to-myofibroblast transition in the old male mouse heart. [Abstract]

2023 Jul 4;26(8):107283. PMID: 37520701
Poultry Sci

SC75741 antagonizes vesicular stomatitis virus, duck Tembusu virus, and duck plague virus infection in duck cells through promoting innate immune responses. [Abstract]

2021 May;100(5):101085. PMID: 33799115
Front Biosci (Landmark Ed)

Activation of the MEK/ERK Pathway Mediates the Inhibitory Effects of Silvestrol on Nasopharyngeal Carcinoma Cells via RAP1A, HK2, and GADD45A. [Abstract]

2024 Apr 23;29(4):160. PMID: 38682208
J Biol Chem

Upregulation of CYR61 by TGF-β and YAP signaling exerts a counter-suppression of hepatocellular carcinoma. [Abstract]

2024 Apr;300(4):107208. PMID: 38521502
Naunyn Schmiedebergs Arch Pharmacol

Label-free cell phenotypic profiling of sphingosine-1-phosphate receptor 1 and discovery of its agonist from natural products. [Abstract]

2026 May 29. PMID: 42209736
Cancer Res Commun

A Drug Discovery Pipeline for MAPK/ERK Pathway Inhibitors in Caenorhabditis elegans. [Abstract]

2024 Sep 1;4(9):2454-2462. PMID: 39212544
J Funct Foods

45 (2018) 110-117.
J Microbiol

Autophagy of bovine mammary epithelial cell induced by intracellular Staphylococcus aureus. [Abstract]

2020 Apr;58(4):320-329. PMID: 32103442
Pathol Res Pract

Effect of NMB-regulated ERK1/2 and p65 signaling pathway on proliferation and apoptosis of cervical cancer. [Abstract]

2022 Oct:238:154104. PMID: 36095918
Arch Med Res

Infiltrating Macrophages Induced Stem-cell-like Features Through PI3K/AKT/GSK3β Signaling to Promote Neurofibroma Growth. [Abstract]

2020 Feb;51(2):124-134. PMID: 32111496
Cancer Med

Metformin revert insulin-induced oxaliplatin resistance by activating mitochondrial apoptosis pathway in human colon cancer HCT116 cells. [Abstract]

2020 Jun;9(11):3875-3884. PMID: 32248666
J Food Biochem

A novel di-peptide Met-Glu from collagen hydrolysates inhibits platelet aggregation and thrombus formation via regulation of Gq-mediated signaling. [Abstract]

2020 Sep;44(9):e13352. PMID: 32662128
Int J Ophthalmol

Blocking VEGF signaling augments interleukin-8 secretion via MEK/ERK/1/2 axis in human retinal pigment epithelial cells. [Abstract]

2020 Jul 18;13(7):1039-1045. PMID: 32685389
Drexel University

2025.
Int J Biol Sci

Cancer-associated adipocytes promote the invasion and metastasis in breast cancer through LIF/CXCLs positive feedback loop. [Abstract]

2022 Jan 16;18(4):1363-1380. PMID: 35280694

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 16.67 mg/mL (36.75 mM; ultrasonic and warming and heat to 60°C; 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

2.2048 mL

11.0239 mL

22.0478 mL

5 mM

0.4410 mL

2.2048 mL

4.4096 mL

10 mM

0.2205 mL

1.1024 mL

2.2048 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

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)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2 mg/mL (4.41 mM); Clear solution

This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2 mg/mL (4.41 mM); Clear solution

This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2 mg/mL (4.41 mM); Clear solution

This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (537 KB)
- English - EN (537 KB)
- Français - FR (537 KB)
- Deutsch - DE (537 KB)
- Norwegian - NO (537 KB)
- Español - ES (537 KB)
- Swedish - SV (537 KB)
- Italian - IT (537 KB)
- Korean - KR (537 KB)
- Portuguese - PT (537 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]. Shripad V. Bhagwat, et al. Abstract 4973: Discovery of LY3214996, a selective and novel ERK1/2 inhibitor with potent antitumor activities in cancer models with MAPK pathway alterations. Cancer Research. July 2017.

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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2048 mL	11.0239 mL	22.0478 mL	55.1195 mL
	5 mM	0.4410 mL	2.2048 mL	4.4096 mL	11.0239 mL
	10 mM	0.2205 mL	1.1024 mL	2.2048 mL	5.5119 mL
	15 mM	0.1470 mL	0.7349 mL	1.4699 mL	3.6746 mL
	20 mM	0.1102 mL	0.5512 mL	1.1024 mL	2.7560 mL
	25 mM	0.0882 mL	0.4410 mL	0.8819 mL	2.2048 mL
	30 mM	0.0735 mL	0.3675 mL	0.7349 mL	1.8373 mL

Keywords

Temuterkib

35 Cited Publications

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Temuterkib

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

Stem Cell Signaling Compound Library

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Bioactive Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) Temuterkib

Alle ERK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (35)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Temuterkib Related Classifications

HY-101494 Related Classifications