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Art. -Nr.: HY-189711

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MTP-B1

MTP-B1 is a POLRMT MtPTAC degrader that activates mitochondrial ClpP. MTP-B1 recruits ClpP as a protease module to POLRMT, inducing ClpP-dependent proteolysis and reducing POLRMT protein levels. MTP-B1 induces ROS and apoptosis. MTP-B1 inhibits proliferation, clonogenic growth, oxidative phosphorylation pathway gene expression, and mitochondrial transcription. MTP-B1 inhibits tumor growth in xenograft tumor mouse models and reduces tumor Ki67. MTP-B1 can be used for pancreatic cancer research (pink: POLRMT inhibitor: HY-181072; blue: small molecule that activates mitochondrial protease ClpP: HY-189815.

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Formel: C₅₂H₅₁F₄N₇O₇
Molecular Weight:962.00

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

MTP-B1 Chemical Structure

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Use of MCE Products

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

Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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Cellular Effect

Cell Line	Type	Value	Description	References
MIA PaCa-2	DC₅₀	187.2 nM	Half-maximal degradation of POLRMT in human MIA PaCa-2 pancreatic cancer cells after 24 hrs incubation by Western blot. Half-maximal degradation of POLRMT in human MIA PaCa-2 pancreatic cancer cells after 24 hrs incubation by Western blot.	42819300
ASPC1	DC₅₀	416.9 nM	Half-maximal degradation of POLRMT in human AsPC-1 pancreatic cancer cells. Half-maximal degradation of POLRMT in human AsPC-1 pancreatic cancer cells.	42819300
MIA PaCa-2	IC50	5.08 nM	Antiproliferative activity against human MIA PaCa-2 pancreatic cancer cells by SRB assay. Antiproliferative activity against human MIA PaCa-2 pancreatic cancer cells by SRB assay.	42819300
ASPC1	IC50	57.76 nM	Antiproliferative activity against human AsPC-1 pancreatic cancer cells by SRB assay. Antiproliferative activity against human AsPC-1 pancreatic cancer cells by SRB assay.	42819300
MIA PaCa-2	DC₅₀	8.81 nM	Half-maximal degradation of POLRMT in human MIA PaCa-2 pancreatic cancer cells after 7 days incubation. Half-maximal degradation of POLRMT in human MIA PaCa-2 pancreatic cancer cells after 7 days incubation.	42819300
MIA PaCa-2	IC50	6.32 nM	Antiproliferative activity against human MIA PaCa-2 pancreatic cancer cells expressing negative control by SRB assay. Antiproliferative activity against human MIA PaCa-2 pancreatic cancer cells expressing negative control by SRB assay.	42819300
MIA PaCa-2	IC50	94.15 nM	Antiproliferative activity against human MIA PaCa-2 pancreatic cancer cells overexpressing POLRMT by SRB assay. Antiproliferative activity against human MIA PaCa-2 pancreatic cancer cells overexpressing POLRMT by SRB assay.	42819300

In Vitro

MTP-B1 (0.5-5 μM and 125-5000 nM; 24 h) potently degrades POLRMT in MIA PaCa-2 cells with a DC₅₀ of 187.2 nM and a D_max of 98.18%; in AsPC-1 cells, the DC₅₀ is 416.9 nM^[1].
MTP-B1 (1 μM; 0-48 h) rapidly degrades POLRMT in MIA PaCa-2 cells, and the degradation persists after compound washout^[1].
MTP-B1 (0.1-1 μM) reduces POLRMT immunofluorescence in MIA PaCa-2 cells in a dose-dependent manner^[1].
MTP-B1 (7 days) exhibits potent antiproliferative activity against MIA PaCa-2 and AsPC-1 cells with IC₅₀ values of 5.08 and 57.76 nM, respectively, and degrades POLRMT with a DC₅₀ of 8.81 nM^[1].
MTP-B1 broadly inhibits OXPHOS gene expression and mitochondrial transcription^[1].
MTP-B1 (1-500 nM) inhibits clonogenic growth of MIA PaCa-2 cells and induces ROS and apoptosis without affecting cell cycle progression or mitochondrial membrane potential^[1].
MTP-B1 (1 μM)-induced POLRMT degradation requires simultaneous binding to both POLRMT and ClpP, and is independent of CRL-dependent ubiquitination and the autophagy-lysosomal pathway^[1].

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

Western Blot Analysis^[1]

Cell Line:

MIA PaCa-2 cells
Concentration:

0.5, 1, 5 μM
Incubation Time:

24 h
Result:

Retained potent POLRMT degradation activity in the initial screen;

Western Blot Analysis^[1]

Cell Line:

MIA PaCa-2 and AsPC-1 cells
Concentration:

125, 250, 500, 1000, 5000 nM
Incubation Time:

24 h
Result:

Dose-response assays gave a DC₅₀ of 187.2 nM and Dmax of 98.18% in MIA PaCa-2 cells.
Showed a DC₅₀ of 416.9 nM in AsPC-1 cells.

Western Blot Analysis^[1]

Cell Line:

MIA PaCa-2 cells
Concentration:

1 μM (time-course); 1 μM for 24 h followed by washout
Incubation Time:

0, 4, 8, 16, 24 h; washout 24 h; 48 h
Result:

MTP-B1 induced more than 50% POLRMT degradation within 16 h and near-complete degradation by 24 h.
A lower-molecular-weight POLRMT species appeared with degradation.
After washout, no appreciable POLRMT recovery was detected within 24 h, with only partial restoration at 48 h.

Parmacokinetics

Species	Dose	Route	C_max	AUC_0-∞	T_1/2
Mice^[1]	50 mg/kg	i.v.	61966.67 ng/mL	26,100.84 ng·h/mL	3.47 h

In Vivo

MTP-B1 (25-100 mg/kg; i.v.; every other day; 25 days) inhibits tumor growth in the MIA PaCa-2 xenograft mice tumor model^[1].

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

Animal Model:

mice with MIA PaCa-2 xenograft^[1]
Dosage:

25, 50, 100 mg/kg
Administration:

i.v.; every other day; 25 days
Result:

Achieved a tumor growth inhibition (TGI) of 70.1% at 100 mg/kg.
No significant body weight
loss.
Exhibited POLRMT degradation, reduced the
proliferation marker Ki67 and significant increased
TUNEL-positive apoptotic cells in tumors.

Related Protocols :

Chemical Information

Molecular Weight 962.00
Formel C₅₂H₅₁F₄N₇O₇
SMILES

O=C(NCCCN(C1=C(CN(CC2=CC=CC(C#N)=C2)CC1)C(N3CC4=CC=C(C(F)(F)F)C=C4)=O)C3=O)CCN5CCN(C([C@H](OC6=CC(O7)=C(C=C6F)C(C8=CC=CC=C8C)=CC7=O)C)=O)CC5
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Chen C, et al. Development of High-Efficiency Mitochondrial Protease Targeting Chimeras (MtPTACs) for Targeted Degradation of POLRMT and Beyond. JACS Au. 2026 Sep 9;6(9):5439-5454. [Content Brief]

Calculators

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)}

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.

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
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MTP-B1

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Beschreibung

Cellular Effect

In Vitro

Parmacokinetics

In Vivo

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

MTP-B1 Related Classifications

HY-189711 Related Classifications

Bioz

Keywords

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