LDC000067
Based on 13 publication(s) in Google Scholar
LDC000067 is a highly specific CDK9 inhibitor with an IC50 value of 44±10 nM in vitro.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.09%
- CAS. Nr.: 1073485-20-7
- Formel: C18H18N4O3S
- Molecular Weight:370.43
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
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Publications Citing Use of MedChemExpress (MCE) LDC000067
More- Nature. 2020 Sep;585(7824):293-297. [Abstract]
- Cell Death Dis. 2025 Dec 8;16(1):881. [Abstract]
- Cell Chem Biol. 2018 Feb 15;25(2):135-142.e5. [Abstract]
- EMBO Mol Med. 2024 Sep;16(9):2132-2145. [Abstract]
- Neoplasia. 2025 Nov:69:101232. [Abstract]
- Cell Signal. 2020 Mar;67:109508. [Abstract]
- Mol Oncol. 2025 Sep 16. [Abstract]
- Biochim Biophys Acta. 2017 Nov 20;1865(2):354-363. [Abstract]
- Toxicol Appl Pharmacol. 2023 Jul 15:471:116568. [Abstract]
- Biochem Biophys Res Commun. 2019 Dec 3;520(2):250-256. [Abstract]
- Biochem Biophys Res Commun. 2019 Jun 11;513(4):967-973. [Abstract]
- Harvard University. 2023 Mar. 30487357.
- bioRxiv. 2019 Oct.
Customer Validation & Images
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WB
Biologische Aktivität
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CDK9- Cyclin T1 44 nM (IC50) |
cdk2-cyclin A 2441 nM (IC50) |
cdk1-cyclin B1 5513 nM (IC50) |
cdk4-cyclin D1 9242 nM (IC50) |
GSK3A 1460 nM (IC50) |
HGK/MAP4K4 820 nM (IC50) |
ABL2/ARG 3640 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| KHOS/NP | IC50 |
6.5 μM
Compound: LDC067; LDC000067
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Cytotoxicity against human KHOS/NP cells assessed as inhibition of cell proliferation incubated for 5 days by MTT assay
Cytotoxicity against human KHOS/NP cells assessed as inhibition of cell proliferation incubated for 5 days by MTT assay
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[PMID: 30579871] |
| Sf9 | IC50 |
3.95 μM
Compound: LDC000067
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Inhibition of CDK1/Cyclin B (unknown origin) expressed in baculoviral infected insect Sf9 cells using histone H1 as substrate in presence of [gamma-33P]ATP
Inhibition of CDK1/Cyclin B (unknown origin) expressed in baculoviral infected insect Sf9 cells using histone H1 as substrate in presence of [gamma-33P]ATP
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[PMID: 26741853] |
| U2OS | IC50 |
5.8 μM
Compound: LDC067; LDC000067
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Cytotoxicity against human U2OS cells assessed as inhibition of cell proliferation incubated for 5 days by MTT assay
Cytotoxicity against human U2OS cells assessed as inhibition of cell proliferation incubated for 5 days by MTT assay
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[PMID: 30579871] |
The selectivity of LDC000067 for CDK9 over other CDKs exceeds that of the known inhibitors flavopiridol and DRB. LDC000067 displayed 55/125/210/ >227/ >227-fold selectivity for CDK9 versus CDK2/1/4/6/7. LDC000067 inhibits in vitro transcription in an ATP-competitive and dose-dependent manner. Gene expression profiling of cells treated with LDC000067 demonstrates a selective reduction of short-lived mRNAs, including important regulators of proliferation and apoptosis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 1073485-20-7
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Appearance Solid
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Molecular Weight 370.43
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Formel C18H18N4O3S
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Color White to off-white
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SMILES
O=S(CC1=CC=CC(NC2=NC=NC(C3=CC=CC=C3OC)=C2)=C1)(N)=O
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Synonyms
LDC067
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (13)
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Journal Impact Factor
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Most Recent
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Nature
2020 Sep;585(7824):293-297. PMID: 32494016 -
Cell Death Dis
Targeting CDK9-dependent transcriptional addiction: a novel chemoprevention strategy for oral carcinogenesis via adenosine deaminase modulation. [Abstract]2025 Dec 8;16(1):881. PMID: 41360777 -
Cell Chem Biol
2018 Feb 15;25(2):135-142.e5. PMID: 29276047 -
EMBO Mol Med
Comprehensive molecular characterization of collecting duct carcinoma for therapeutic vulnerability. [Abstract]2024 Sep;16(9):2132-2145. PMID: 39122888 -
Neoplasia
2025 Nov:69:101232. PMID: 40975978 -
Cell Signal
2020 Mar;67:109508. PMID: 31866490 -
Mol Oncol
Inhibition of CDK9 enhances AML cell death induced by combined venetoclax and azacitidine. [Abstract]2025 Sep 16. PMID: 40955793 -
Biochim Biophys Acta
Selective inhibition reveals cyclin-dependent kinase 2 as another kinase that phosphorylates the androgen receptor at serine 81. [Abstract]2017 Nov 20;1865(2):354-363. PMID: 29157894
LDC000067 purchased from MedChemExpress. Usage Cited in: Biochim Biophys Acta. 2017 Nov 20;1865(2):354-363. [Abstract]
LAPC-4 cells are grown in charcoal-stripped serum medium (CSS) for 24 hours and then stimulated by R1881 alone or with different doses of LDC000067. LDC000067 is added 30 min before androgen treatment. Cellular expression of all proteins was detected by immunoblotting analysis. β-actin was included as a control for protein loading.
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Toxicol Appl Pharmacol
Inhibition of CDK9 exhibits anticancer activity in hepatocellular carcinoma cells via targeting ribonucleotide reductase. [Abstract]2023 Jul 15:471:116568. PMID: 37245555 -
Biochem Biophys Res Commun
2019 Dec 3;520(2):250-256. PMID: 31594641 -
Biochem Biophys Res Commun
2019 Jun 11;513(4):967-973. PMID: 31005255 -
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Lösungsmittel & Löslichkeit
DMSO : ≥ 47 mg/mL (126.88 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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.
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.75 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.75 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
The fluorescence resonance energy transfer (FRET)-based LANCE Ultra KinaSelect Ser/Thr kit is used to determine IC50 values for various CDK inhibitors. Briefly, a specific ULight MBP peptide substrate (50 nM final concentration) is phosphorylated by a CDK-cyclin pair in buffer (50 mM HEPES-KOH pH 7.5, 10 mM MgCl2, 1 mM EGTA, 2 mM dithiothreitol) containing ATP at the concentration of the Km values of the individual kinases for 1 h at room temperature. Subsequently, phosphorylation is detected by addition of specific Eu-labelled anti-phospho-antibodies (2 nM), which upon binding to the phosphopeptide give rise to a FRET signal. FRET signals are then recorded[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (275 KB)
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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)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
Complete Stock Solution Preparation Table
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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6996 mL | 13.4978 mL | 26.9957 mL | 67.4891 mL |
| 5 mM | 0.5399 mL | 2.6996 mL | 5.3991 mL | 13.4978 mL | |
| 10 mM | 0.2700 mL | 1.3498 mL | 2.6996 mL | 6.7489 mL | |
| 15 mM | 0.1800 mL | 0.8999 mL | 1.7997 mL | 4.4993 mL | |
| 20 mM | 0.1350 mL | 0.6749 mL | 1.3498 mL | 3.3745 mL | |
| 25 mM | 0.1080 mL | 0.5399 mL | 1.0798 mL | 2.6996 mL | |
| 30 mM | 0.0900 mL | 0.4499 mL | 0.8999 mL | 2.2496 mL | |
| 40 mM | 0.0675 mL | 0.3374 mL | 0.6749 mL | 1.6872 mL | |
| 50 mM | 0.0540 mL | 0.2700 mL | 0.5399 mL | 1.3498 mL | |
| 60 mM | 0.0450 mL | 0.2250 mL | 0.4499 mL | 1.1248 mL | |
| 80 mM | 0.0337 mL | 0.1687 mL | 0.3374 mL | 0.8436 mL | |
| 100 mM | 0.0270 mL | 0.1350 mL | 0.2700 mL | 0.6749 mL |
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