LDC000067

For research use only.

Catalog No.S7461 Synonyms: LDC067

28 publications

CAS No. 1073485-20-7

LDC000067 (LDC067) is a highly selective CDK9 inhibitor with IC50 of 44 nM, 55/125/210/ >227/ >227-fold selectivity over CDK2/1/4/6/7.

Selleck's LDC000067 has been cited by 28 publications

Nature, 2019, 10.1038/s41586-019-1607-3

PubMed: 31578521 ( click the link to review the publication )

Cancer Discov, 2019, 10.1158/2159-8290

PubMed: 31466944 ( click the link to review the publication )

Mol Cell, 2020, 77(6):1322-1339

PubMed: 32006464 ( click the link to review the publication )

Cell Rep, 2020, 7;31(1):107485

PubMed: 32268092 ( click the link to review the publication )

Cancers (Basel), 2020, 12(6):E1637

PubMed: 32575711 ( click the link to review the publication )

Cell Death Dis, 2020, 11(7):538

PubMed: 32678076 ( click the link to review the publication )

Sci Adv, 2020, 6(29):eaba1593

PubMed: 32832621 ( click the link to review the publication )

J Cancer, 2020, 11(1):132-141

PubMed: 31892980 ( click the link to review the publication )

Nucleic Acids Res, 2020, 48(2):633-645

PubMed: 31777926 ( click the link to review the publication )

Cell Signal, 2020, 67:109508

PubMed: 31866490 ( click the link to review the publication )

Mol Cell, 2019, 74(4):674-687

PubMed: 30928206 ( click the link to review the publication )

Dev Cell, 2019, 51(1):35-48.e7

PubMed: 31422918 ( click the link to review the publication )

FASEB J, 2019, 33(5):5990-6000

PubMed: 30726104 ( click the link to review the publication )

Front Immunol, 2019, 10:1718

PubMed: 31402912 ( click the link to review the publication )

J Virol, 2019, 93(12)

PubMed: 30971469 ( click the link to review the publication )

Biochem Pharmacol, 2019, 171:113691

PubMed: 31704236 ( click the link to review the publication )

Biochem Biophys Res Commun, 2019, 520(2):250-256

PubMed: 31594641 ( click the link to review the publication )

Biochem Biophys Res Commun, 2019, 10.1016/j.bbrc.2019.07.032

PubMed: 31307784 ( click the link to review the publication )

Mol Cancer Ther, 2019, 10.1158/1535-7163.MCT-19-0451

PubMed: 31744894 ( click the link to review the publication )

Oncogene, 2018, 37(21):2850-2862

PubMed: 29511348 ( click the link to review the publication )

Sci Rep, 2018, 8(1):11554

PubMed: 30068949 ( click the link to review the publication )

J Orthop Res, 2018, 10.1002/jor.24189

PubMed: 30488489 ( click the link to review the publication )

Hum Mol Genet, 2017, 10.1093/hmg/ddx233

PubMed: 28637276 ( click the link to review the publication )

Oncotarget, 2017, 8(63):107206-107222

PubMed: 29291023 ( click the link to review the publication )
Reprod Biol, 2017, 17(4):320-326

PubMed: 28935119 ( click the link to review the publication )

PLoS Pathog, 2016, 12(10):e1005950

PubMed: 27764245 ( click the link to review the publication )

Oncotarget, 2016, 7(36):58051-58064

PubMed: 27517323 ( click the link to review the publication )

Kidney Int, 2015, 88(6):1323-1335

PubMed: 26221756 ( click the link to review the publication )

Purity & Quality Control

Choose Selective CDK Inhibitors

Biological Activity

Description

LDC000067 (LDC067) is a highly selective CDK9 inhibitor with IC50 of 44 nM, 55/125/210/ >227/ >227-fold selectivity over CDK2/1/4/6/7.

Features

CDK9-selective inhibitor.

Targets

CDK9 ^[1] (Cell-free assay)	CDK2 ^[1] (Cell-free assay)
44 nM	2.441 μM

In vitro

LDC000067 reduces Ser2-P, induces p53 activation and leads to apoptosis in mESCs. In addition, LDC067 also dose-dependently inhibits P-TEFb-dependent de novo RNA synthesis of cellular genes.^[1]

Assay

Methods	Test Index	PMID
Western blot	CDK9 / RNAPII / p-RNAPII / MCL-1 / BIRC5; PubMed: 30579871 EBioMedicine (D) The expression of proteins involved in the CDK9-signaling pathway in the U2OS osteosarcoma cell line was examined by Western blotting after 48 h of LDC067 treatment. (E) Semiquantitative analysis of (D) densitometry relative to tubulin. The data represent the mean ± SE of the experiment carried out in triplicate. (F) The expression of proteins involved in the CDK9-signaling pathway in the KHOS osteosarcoma cell line was examined by Western blotting after 48 h of LDC067 treatment. (G) Semiquantitative analysis of (F) densitometry relative to tubulin. The data are mean ± SE of the experiment carried out in triplicate.	30579871

Protocol

References

[1] Albert TK, et al. Br J Pharmacol. 2014, 171(1), 55-68.

Solubility (25°C)

In vitro	DMSO	74 mg/mL (199.76 mM)
	Water	Insoluble
	Ethanol	Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information Download LDC000067 SDF

Molecular Weight	370.43
Formula	C₁₈H₁₈N₄O₃S
CAS No.	1073485-20-7
Storage	3 years-20°C powder 2 years-80°C in solvent
Synonyms	LDC067
Smiles	COC1=CC=CC=C1C2=CC(=NC=N2)NC3=CC=CC(=C3)CS(=O)(=O)N

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)

% DMSO+ % + % Tween 80+ % ddH₂O

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Calculation results:

Working concentration： mg/ml；

Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL， Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH₂O，mix and clarify.

Note：1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Bio Calculators

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

Serial Dilutions
Concertration (start):
Dilution-folds:

Computed Result

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

CDK Signaling Pathway Map

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LDC000067