LDC000067
- CAS NO.:1073485-20-7
- Empirical Formula: C18H18N4O3S
- Molecular Weight: 370.43
- MDL number: MFCD28137788
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-07-02 08:55:00
What is LDC000067?
Biological Activity
ldc000067 (ldc067) is a novel specific inhibitor of cdk9 with ic50 value of 44 ± 10 nm [1].cyclin-dependent kinase 9 (cdk9) is a cyclin-dependent kinase. cdk9 and cyclin t form the positive transcription elongation factor b (p-tefb) complex for rna polymerase ii and functions by phosphorylating the c-terminal domain of the largest subunit of rna polymerase ii [1].ldc000067 (ldc067) is a novel and highly specific cdk9 inhibitor. ldc000067 exhibited selectivity for cdk9 over other cdks in the range of 55-fold (vs. cdk2) to over 230-fold (vs. cdk6 and cdk7). ldc067 also inhibited transcription in a dose-dependent and atp-competitive manner. in whole cells, ldc000067 induced the tumor suppressor protein p53 activation and apoptosis. ldc000067 also selectively reduced short-lived mrnas, including those that encode regulators of apoptosis and proliferation such as myc and mcl1 [1].
in vitro
LDC000067 reduces Ser2-P in mESCs, induces p53 activation, and leads to apoptosis. In addition, LDC067 also dose-dependently inhibited the de novo RNA synthesis of P-TEFb-dependent cellular genes.
storage
Store at -20°C
References
[1]. albert tk, rigault c, eickhoff j, et al. characterization of molecular and cellular functions of the cyclin-dependent kinase cdk9 using a novel specific inhibitor. br j pharmacol, 2014, 171(1): 55-68.
Properties of LDC000067
Boiling point: | 604.1±65.0 °C(Predicted) |
Density | 1.360±0.06 g/cm3(Predicted) |
storage temp. | under inert gas (nitrogen or Argon) at 2–8 °C |
solubility | insoluble in H2O; insoluble in EtOH; ≥18.52 mg/mL in DMSO |
form | Powder |
pka | 10.27±0.60(Predicted) |
color | White to off-white |
Safety information for LDC000067
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H302:Acute toxicity,oral H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation H335:Specific target organ toxicity, single exposure;Respiratory tract irritation |
Precautionary Statement Codes |
P261:Avoid breathing dust/fume/gas/mist/vapours/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. |
Computed Descriptors for LDC000067
New Products
Tubulysin B Tubulysin H 2,2-diethoxyethanethioamide Tubulysin D Diethyl Aluminium Cyanide (1.0 M in Toluene) 3-METHYLAZETIDIN-3-OL HYDROCHLORIDE 1,2,3,6-TETRAHYDROPYRIDINE HYDROCHLORIDE tetrahydro-4-methyl-2H-pyran 3-Aminocyclobutanone hydrochloride CYCLOBUTYLAMINE HYDROCHLORIDE 4,4-DIFLUOROPIPERIDINE 2-[2-[3(S)-3[2-(7-chloro-2-quinolinyl) ethenyl] phenyl-3- hydroxyl propyl] phenyl]-2-propanol Imeglimin Hydrochloride IH 2-[[(3aR,4S,6R,6aS)-6-Aminotetrahydro-2,2-dimethyl-4H-cyclopenta-1,3-dioxol-4-yl]oxy]ethanol ethanedioate 2-(1-(Mercaptomethyl) cyclopropyl) acetonitrile (1R,2S)-2-(3,4-Difluorophenyl)cyclopropanamine Calcium Sodium Phosphosilicate IH (R)-1-Aminoindan Hydrochloride (2,3-Dihydro- benzofuran-5-yl)- ethanol Magnesium Trisilicate Lubiprostone Latanoprostene Bunod Flame Retardant Zinc Borate 1H-Imidazole-4-carbonitrileRelated products of tetrahydrofuran
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