Referencia número: HY-137067

IMT1B

(Synonyms: LDC203974)

10 Cited Publications

Revisión del cliente

Based on 10 publication(s) in Google Scholar

IMT1B (LDC203974) is an orally active, noncompetitive and specific allosteric inhibitor of mitochondrial RNA polymerase (POLRMT) and inhibits mitochondrial DNA (mtDNA) expression. IMT1B has anti-tumour effects.

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Pureza: 99.45%
No. CAS: 2304621-06-3
Fòrmula: C₂₄H₂₁ClFNO₆
Peso molecular:473.88

Almacenamiento:

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

IMT1B Chemical Structure

No. CAS: 2304621-06-3

Tamaño

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Sample (0.1mg)

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(In Japan)

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (10)
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target

RNA Polymerase

Ver todos los productos específicos de isoformas DNA/RNA Synthesis :

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	0.138 μM Compound: IMT1B	Antiproliferative activity against human A2780 cells incubated for 168 hrs by SRB method Antiproliferative activity against human A2780 cells incubated for 168 hrs by SRB method	[PMID: 36997840]
A549	IC₅₀	0.881 μM Compound: IMT1B	Antiproliferative activity against human A549 cells incubated for 168 hrs by SRB method Antiproliferative activity against human A549 cells incubated for 168 hrs by SRB method	[PMID: 36997840]
CAPAN-1	IC₅₀	1.352 μM Compound: IMT1B	Antiproliferative activity against human CAPAN-1 cells assessed as cell viability measured after 168 hrs incubation by SRB assay Antiproliferative activity against human CAPAN-1 cells assessed as cell viability measured after 168 hrs incubation by SRB assay	[PMID: 39049433]
DLD-1	IC₅₀	0.142 μM Compound: IMT1B	Antiproliferative activity against human DLD-1 cells incubated for 168 hrs by SRB method Antiproliferative activity against human DLD-1 cells incubated for 168 hrs by SRB method	[PMID: 36997840]
HeLa	IC₅₀	1.052 μM Compound: IMT1B	Antiproliferative activity against human HeLa cells incubated for 168 hrs by SRB method Antiproliferative activity against human HeLa cells incubated for 168 hrs by SRB method	[PMID: 36997840]
HepG2	IC₅₀	0.168 μM Compound: IMT1B	Antiproliferative activity against human HepG2 cells incubated for 168 hrs by SRB method Antiproliferative activity against human HepG2 cells incubated for 168 hrs by SRB method	[PMID: 36997840]
HUVEC	IC₅₀	>50 μM Compound: IMT1B	Antiproliferative activity against HUVEC cells assessed as cell viability measured after 168 hrs incubation by SRB assay Antiproliferative activity against HUVEC cells assessed as cell viability measured after 168 hrs incubation by SRB assay	[PMID: 39049433]
IMR-90	IC₅₀	>50 μM Compound: IMT1B	Antiproliferative activity against human IMR-90 cells incubated for 168 hrs by SRB method Antiproliferative activity against human IMR-90 cells incubated for 168 hrs by SRB method	[PMID: 36997840]
MDA-MB-231	IC₅₀	>10 μM Compound: IMT1B	Antiproliferative activity against human MDA-MB-231 cells incubated for 168 hrs by SRB method Antiproliferative activity against human MDA-MB-231 cells incubated for 168 hrs by SRB method	[PMID: 36997840]
MDA-MB-468	IC₅₀	0.189 μM Compound: IMT1B	Antiproliferative activity against human MDA-MB-468 cells incubated for 168 hrs by SRB method Antiproliferative activity against human MDA-MB-468 cells incubated for 168 hrs by SRB method	[PMID: 36997840]
MIA PaCa-2	IC₅₀	0.152 μM Compound: IMT1B	Antiproliferative activity against human MIA PaCa-2 cells incubated for 168 hrs by SRB method Antiproliferative activity against human MIA PaCa-2 cells incubated for 168 hrs by SRB method	[PMID: 36997840]
MIA PaCa-2	IC₅₀	0.159 μM Compound: IMT1B	Antiproliferative activity against human MIA PaCa-2 cells assessed as cell viability measured after 168 hrs incubation by SRB assay Antiproliferative activity against human MIA PaCa-2 cells assessed as cell viability measured after 168 hrs incubation by SRB assay	[PMID: 39049433]
NCI-H1975	IC₅₀	0.221 μM Compound: IMT1B	Antiproliferative activity against human NCI-H1975 cells incubated for 168 hrs by SRB method Antiproliferative activity against human NCI-H1975 cells incubated for 168 hrs by SRB method	[PMID: 36997840]
NCI-H3122	IC₅₀	>10 μM Compound: IMT1B	Antiproliferative activity against human NCI-H3122 cells incubated for 168 hrs by SRB method Antiproliferative activity against human NCI-H3122 cells incubated for 168 hrs by SRB method	[PMID: 36997840]
PANC-1	IC₅₀	1.566 μM Compound: IMT1B	Antiproliferative activity against human PANC-1 cells assessed as cell viability measured after 168 hrs incubation by SRB assay Antiproliferative activity against human PANC-1 cells assessed as cell viability measured after 168 hrs incubation by SRB assay	[PMID: 39049433]
PBMC	IC₅₀	>50 μM Compound: IMT1B	Antiproliferative activity against human PBMC cells incubated for 168 hrs by SRB method Antiproliferative activity against human PBMC cells incubated for 168 hrs by SRB method	[PMID: 36997840]

In Vitro

IMT1B is a noncompetitive inhibitor that causes a conformational change of POLRMT, which blocks substrate binding and transcription in a dose-dependent way in vitro^[1].
IMT1B (0.01 nM-10 μM; 72-168 hours) dose-dependently decreases in cell viability in A2780, A549 and HeLa cells^[1].
IMT1B depletes cellular metabolites^[1].
IMT1B increases the levels of mono- and diphosphate nucleotides that results in a considerable increase in the AMP/ATP ratio and levels of phosphorylated AMPK^[1].

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

Cell Viability Assay^[1]

Cell Line:

A2780 cells
Concentration:

0.01 nM, 1 nM, 10 nM, 100 nM, 1 μM, 10 μM
Incubation Time:

72 hours, 96 hours, 168 hours
Result:

Decreased cell viability in a dose-dependent manner.

In Vivo

IMT1B (100 mg/kg; p.o.; daily; for four weeks) significantly reduces tumour size in mice containing xenografts^[1].
IMT1B reduces mtDNA transcript levels and respiratory-chain subunit levels in tumours^[1].
IMT1B exhibits good oral bioavailability (mice 101 %) and C_max (mice 5149 ng/mL) following oral administration (mice 10 mg/kg)^[1].
IMT1B exhibits elimination half-life (mice 1.88 h) due to plasma clearance (mice 0.44 L/h/kg) following intravenous administration (mice 1 mg/kg)^[1].

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

Animal Model:

7-9 weeks female BALB/c nude mice, with A2780 cells xenograft^[1]
Dosage:

100 mg/kg
Administration:

Oral administration, daily, for four weeks
Result:

Led to a clear reduction of tumour volume.

Animal Model:

Mice^[1]
Dosage:

1 mg/kg for i.v.; 10 mg/kg for oral (Pharmacokinetic Analysis)
Administration:

Intravenous administration and oral administration
Result:

Oral bioavailability (101%), C_max (5149 ng/mL), T_1/2 (1.88 h).

Chemical Information

No. CAS 2304621-06-3
Appearance Solid
Peso molecular 473.88
Fòrmula C₂₄H₂₁ClFNO₆
Color White to off-white
SMILES

O=C([C@@H]1CN(C([C@H](OC2=CC=C(C(O3)=C2)C(C4=CC=C(F)C=C4Cl)=CC3=O)C)=O)CCC1)O
Synonyms

LDC203974
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

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

Publications (10)

All RT-PCRIFWB

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Journal Impact Factor

Cell Metab

A novel protein CYTB-187AA encoded by the mitochondrial gene CYTB modulates mammalian early development. [Abstract]

2024 Jul 2;36(7):1586-1597.e7. PMID: 38703762
Nat Cell Biol

Regulators of mitonuclear balance link mitochondrial metabolism to mtDNA expression. [Abstract]

2023 Nov;25(11):1575-1589. PMID: 37770567

IMT1B purchased from MedChemExpress. Usage Cited in: Nat Cell Biol. 2023 Nov;25(11):1575-1589. [Abstract]

qRT-PCR measurements of MT-CO1 mRNA levels after treatment with IMT1B (500nM) for indicated time in NT or NME6 KO K562 cells.
Nat Commun

Oncogenic KRAS-driven type I interferon signalling primes pancreatic cancer for necroptosis. [Abstract]

2026 Jun 15;17(1):5288. PMID: 42297776
Exp Mol Med

Nucleus pulposus cells regulate macrophages in degenerated intervertebral discs via the integrated stress response-mediated CCL2/7-CCR2 signaling pathway. [Abstract]

2024 Feb;56(2):408-421. PMID: 38316963

IMT1B purchased from MedChemExpress. Usage Cited in: Exp Mol Med. 2024 Feb;56(2):408-421. [Abstract]

Immunofluorescence staining of dsRNA and mitochondria in rNPCs pretreated with TLR4-IN-C34, MitoTempo or IMT1B (200 nM) for 1 h and then treated with LPS for 6 h.

IMT1B purchased from MedChemExpress. Usage Cited in: Exp Mol Med. 2024 Feb;56(2):408-421. [Abstract]

cl2 and Ccl7 gene expression in rNPCs with or without IMT1B (200 nM) pretreatment for 1 h and LPS treatment for 6 h.

IMT1B purchased from MedChemExpress. Usage Cited in: Exp Mol Med. 2024 Feb;56(2):408-421. [Abstract]

IMT1B (200 nM) pretreatment for 1 h and LPS treatment for 6 h. The expression of PKR-ISR pathway-related proteins in rNPCs.
Cell Death Discov

Identification of a novel minor-groove DNA binder that represses mitochondrial gene expression and induces apoptosis in highly aggressive leiomyosarcoma cells. [Abstract]

2025 Nov 10;11(1):524. PMID: 41213941

IMT1B purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2025 Nov 10;11(1):524. [Abstract]

Expression levels of the indicated mitochondrial encoded genes in SK-UT-1 cells treated with10 µM of XMH95, Hoechst 33258 or IMT1B. Incubation time was 18 hours for XMH95 and Hoechst 33258, and 48 hours for IMT1B. RNAs were extracted at the indicated processed for qRT-PCR.
Int Immunopharmacol

STING-mediated mitochondrial DNA release exacerbates PANoptosis in liver ischemia reperfusion injury. [Abstract]

2025 May 7:157:114778. PMID: 40339491
Int Immunopharmacol

mtDNA/RNA boosts radiation-induced abscopal effect via M1 macrophage polarization-promoted IFN-β-dependent inflammatory response. [Abstract]

2025 Apr 16:155:114673. PMID: 40245773
Mol Biol Cell

The mitochondrial RNA granule modulates manganese-dependent cell toxicity. [Abstract]

2022 Oct 1;33(12):ar108. PMID: 35921164
SSRN

2025 Dec 15.
bioRxiv

January 04, 2022.

Solvente y solubilidad

In Vitro:

DMSO : 200 mg/mL (422.05 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

2.1102 mL

10.5512 mL

21.1024 mL

5 mM

0.4220 mL

2.1102 mL

4.2205 mL

10 mM

0.2110 mL

1.0551 mL

2.1102 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.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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: ≥ 5 mg/mL (10.55 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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% Corn Oil

Solubility: ≥ 5 mg/mL (10.55 mM); Clear solution

This protocol yields a clear solution of ≥ 5 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 (50.0 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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (277 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 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)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Nina A Bonekamp, et al. Small-molecule inhibitors of human mitochondrial DNA transcription. Nature. 2020 Dec;588(7839):712-716. [Content Brief]

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	2.1102 mL	10.5512 mL	21.1024 mL	52.7560 mL
	5 mM	0.4220 mL	2.1102 mL	4.2205 mL	10.5512 mL
	10 mM	0.2110 mL	1.0551 mL	2.1102 mL	5.2756 mL
	15 mM	0.1407 mL	0.7034 mL	1.4068 mL	3.5171 mL
	20 mM	0.1055 mL	0.5276 mL	1.0551 mL	2.6378 mL
	25 mM	0.0844 mL	0.4220 mL	0.8441 mL	2.1102 mL
	30 mM	0.0703 mL	0.3517 mL	0.7034 mL	1.7585 mL
	40 mM	0.0528 mL	0.2638 mL	0.5276 mL	1.3189 mL
	50 mM	0.0422 mL	0.2110 mL	0.4220 mL	1.0551 mL
	60 mM	0.0352 mL	0.1759 mL	0.3517 mL	0.8793 mL
	80 mM	0.0264 mL	0.1319 mL	0.2638 mL	0.6594 mL
	100 mM	0.0211 mL	0.1055 mL	0.2110 mL	0.5276 mL

IMT1B

10 Cited Publications

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IMT1B

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Orally Active Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) IMT1B

Ver todos los productos específicos de isoformas DNA/RNA Synthesis

Actividad biológica

Chemical Information

Publications (10)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

IMT1B

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Orally Active Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) IMT1B

Ver todos los productos específicos de isoformas DNA/RNA Synthesis

Actividad biológica

Chemical Information

Publications (10)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

IMT1B Related Classifications

Referencia número: HY-137067