NSC-636819 | CAS#1618672-71-1 | KDM4A/KDM4B inhibitor

MedKoo Cat#: 527664 | Name: NSC-636819

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

NSC-636819 is a novel KDM4A/KDM4B inhibitor.

Chemical Structure

NSC-636819

CAS#1618672-71-1

Theoretical Analysis

MedKoo Cat#: 527664

Name: NSC-636819

CAS#: 1618672-71-1

Chemical Formula: C22H12Cl4N2O4

Exact Mass: 507.9551

Molecular Weight: 510.15

Elemental Analysis: C, 51.80; H, 2.37; Cl, 27.80; N, 5.49; O, 12.54

Price and Availability

Size	Price	Availability	Quantity
10mg	USD 400.00	2 Weeks
50mg	USD 1,360.00	2 Weeks

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Related CAS #

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Synonym

NSC 636819; NSC636819; NSC-636819

IUPAC/Chemical Name

1,5-Bis[(1E)-2-(3,4-dichlorophenyl)ethenyl]-2,4-dinitrobenzene

InChi Key

YYZPXBXVBQSBDG-IJIVKGSJSA-N

InChi Code

InChI=1S/C22H12Cl4N2O4/c23-17-7-3-13(9-19(17)25)1-5-15-11-16(22(28(31)32)12-21(15)27(29)30)6-2-14-4-8-18(24)20(26)10-14/h1-12H/b5-1+,6-2+

SMILES Code

O=[N+](C1=C(/C=C/C2=CC=C(Cl)C(Cl)=C2)C=C(/C=C/C3=CC=C(Cl)C(Cl)=C3)C([N+]([O-])=O)=C1)[O-]

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

NSC636819 is a competitive and selective inhibitor of KDM4A/KDM4B.

In vitro activity:

Further kinetic inhibition characterization of compound 4 (NSC636819) demonstrated a competitive inhibitory mode against H33–17K9me3 for KDM4A [IC50 = 6.4 μM; Ki (H3K9me3) = 5.5 ± 1.6 μM; Figure 3B). This study further characterized the methylated status of H3 in LNCaP cells treated with compound 4. As shown in Figure S4B, only the level of H3K9me3 was significantly increased in compound 4-treated LNCaP cells as opposed to essentially comparable signals of H3K4me2, H3K27me3, H3K27me2, H3K36me3, H3K36me2, and H3K79me2 between control and treated cells. Reference: J Med Chem. 2014 Jul 24;57(14):5975-85. https://pubmed.ncbi.nlm.nih.gov/24971742/

In vivo activity:

TBD

	Solvent	mg/mL	mM
Solubility
	DMSO	5.1	10.00

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 510.15 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

Chu CH, Wang LY, Hsu KC, Chen CC, Cheng HH, Wang SM, Wu CM, Chen TJ, Li LT, Liu R, Hung CL, Yang JM, Kung HJ, Wang WC. KDM4B as a target for prostate cancer: structural analysis and selective inhibition by a novel inhibitor. J Med Chem. 2014 Jul 24;57(14):5975-85. doi: 10.1021/jm500249n. Epub 2014 Jul 9. PMID: 24971742; PMCID: PMC4216216.

In vitro protocol:

In vivo protocol:

TBD

1: Chu CH, Wang LY, Hsu KC, Chen CC, Cheng HH, Wang SM, Wu CM, Chen TJ, Li LT, Liu R, Hung CL, Yang JM, Kung HJ, Wang WC. KDM4B as a target for prostate cancer: structural analysis and selective inhibition by a novel inhibitor. J Med Chem. 2014 Jul 24;57(14):5975-85. doi: 10.1021/jm500249n. Epub 2014 Jul 9. PubMed PMID: 24971742; PubMed Central PMCID: PMC4216216.