JQ-EZ-05 | JQEZ5 | CAS#1913252-04-6 | EZH2 inhibitor

MedKoo Cat#: 540228 | Name: JQ-EZ-05

Description:

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

JQ-EZ-05, also known as JQEZ5 is a Potent and selective SAM-competitive EZH2 inhibitor (IC50 = 11 nM). JQ-EZ-05 selectively binds EZH2 over a panel of 22 methyltransferases.

Chemical Structure

JQ-EZ-05

CAS#1913252-04-6

Theoretical Analysis

MedKoo Cat#: 540228

Name: JQ-EZ-05

CAS#: 1913252-04-6

Chemical Formula: C30H38N8O2

Exact Mass: 542.3118

Molecular Weight: 542.69

Elemental Analysis: C, 66.40; H, 7.06; N, 20.65; O, 5.90

Price and Availability

Size	Price	Availability
50mg	USD 450.00	2 Weeks
100mg	USD 750.00	2 Weeks
200mg	USD 1,350.00	2 Weeks
500mg	USD 2,850.00	2 Weeks
1g	USD 3,850.00	2 Weeks
2g	USD 6,450.00	2 Weeks

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Synonym

JQEZ5; JQEZ-5; JQEZ 5; JQ-EZ-05; JQ-EZ05; JQ-EZ 05;

IUPAC/Chemical Name

1-isopropyl-N-((6-methyl-2-oxo-4-propyl-1,2-dihydropyridin-3-yl)methyl)-6-(6-(4-methylpiperazin-1-yl)pyridin-3-yl)-1H-pyrazolo[3,4-b]pyridine-4-carboxamide

InChi Key

LQTWDAYNGMMHLV-UHFFFAOYSA-N

InChi Code

InChI=1S/C30H38N8O2/c1-6-7-21-14-20(4)34-30(40)24(21)17-32-29(39)23-15-26(35-28-25(23)18-33-38(28)19(2)3)22-8-9-27(31-16-22)37-12-10-36(5)11-13-37/h8-9,14-16,18-19H,6-7,10-13,17H2,1-5H3,(H,32,39)(H,34,40)

SMILES Code

CC(C)N1N=CC2=C(C=C(N=C12)C3=CC=C(N4CCN(CC4)C)N=C3)C(NCC5=C(CCC)C=C(C)NC5=O)=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:

JQEZ5 is a potent and selective EZH2 lysine methyltransferase inhibitor. JQEZ5 SAM-competitive inhibition of polycomb repressive complex 2 (PRC2) with an IC50 of 80 nM.

In vitro activity:

JQEZ5 and UNC1999 inhibited colony formation of primary human CD34+ CML stem/progenitor cells (Fig. 2D–E and Supplementary Fig. 3E–F). Reference: Cancer Discov. 2016 Nov;6(11):1237-1247. https://pubmed.ncbi.nlm.nih.gov/27630126/

In vivo activity:

Tumor-bearing mice were then treated with JQEZ5 for three weeks (75 mg/kg IP daily) and the tumor volume of the lungs was comparatively visualized by MRI. Animals treated with JQEZ5 exhibited rapid and pronounced tumor regression over the three week treatment course, as demonstrated by two-dimensional MRI and volumetric measurements (Figure 7C). Reference: Cancer Discov. 2016 Sep;6(9):1006-21. https://pubmed.ncbi.nlm.nih.gov/27312177/

	Solvent	mg/mL	mM	comments
Solubility
	DMSO	17.9	33.03

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 542.69 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:

1. Xie H, Peng C, Huang J, Li BE, Kim W, Smith EC, Fujiwara Y, Qi J, Cheloni G, Das PP, Nguyen M, Li S, Bradner JE, Orkin SH. Chronic Myelogenous Leukemia- Initiating Cells Require Polycomb Group Protein EZH2. Cancer Discov. 2016 Nov;6(11):1237-1247. doi: 10.1158/2159-8290.CD-15-1439. Epub 2016 Sep 14. PMID: 27630126; PMCID: PMC5096974. 2. Zhang H, Qi J, Reyes JM, Li L, Rao PK, Li F, Lin CY, Perry JA, Lawlor MA, Federation A, De Raedt T, Li YY, Liu Y, Duarte MA, Zhang Y, Herter-Sprie GS, Kikuchi E, Carretero J, Perou CM, Reibel JB, Paulk J, Bronson RT, Watanabe H, Brainson CF, Kim CF, Hammerman PS, Brown M, Cichowski K, Long H, Bradner JE, Wong KK. Oncogenic Deregulation of EZH2 as an Opportunity for Targeted Therapy in Lung Cancer. Cancer Discov. 2016 Sep;6(9):1006-21. doi: 10.1158/2159-8290.CD-16-0164. Epub 2016 Jun 16. PMID: 27312177; PMCID: PMC5010480.

In vitro protocol:

In vivo protocol:

1. Zhang H, Qi J, Reyes JM, Li L, Rao PK, Li F, Lin CY, Perry JA, Lawlor MA, Federation A, De Raedt T, Li YY, Liu Y, Duarte MA, Zhang Y, Herter-Sprie GS, Kikuchi E, Carretero J, Perou CM, Reibel JB, Paulk J, Bronson RT, Watanabe H, Brainson CF, Kim CF, Hammerman PS, Brown M, Cichowski K, Long H, Bradner JE, Wong KK. Oncogenic Deregulation of EZH2 as an Opportunity for Targeted Therapy in Lung Cancer. Cancer Discov. 2016 Sep;6(9):1006-21. doi: 10.1158/2159-8290.CD-16-0164. Epub 2016 Jun 16. PMID: 27312177; PMCID: PMC5010480.

1: Frankel AE, Liu X, Minna JD. Developing EZH2-Targeted Therapy for Lung Cancer. Cancer Discov. 2016 Sep;6(9):949-52. doi: 10.1158/2159-8290.CD-16-0800. PMID: 27587466; PMCID: PMC5012289. 2: Zhang H, Qi J, Reyes JM, Li L, Rao PK, Li F, Lin CY, Perry JA, Lawlor MA, Federation A, De Raedt T, Li YY, Liu Y, Duarte MA, Zhang Y, Herter-Sprie GS, Kikuchi E, Carretero J, Perou CM, Reibel JB, Paulk J, Bronson RT, Watanabe H, Brainson CF, Kim CF, Hammerman PS, Brown M, Cichowski K, Long H, Bradner JE, Wong KK. Oncogenic Deregulation of EZH2 as an Opportunity for Targeted Therapy in Lung Cancer. Cancer Discov. 2016 Sep;6(9):1006-21. doi: 10.1158/2159-8290.CD-16-0164. Epub 2016 Jun 16. PMID: 27312177; PMCID: PMC5010480. 3: He Z, Zhang S, Ma D, Fang Q, Yang L, Shen S, Chen Y, Ren L, Wang J. HO-1 promotes resistance to an EZH2 inhibitor through the pRB-E2F pathway: correlation with the progression of myelodysplastic syndrome into acute myeloid leukemia. J Transl Med. 2019 Nov 11;17(1):366. doi: 10.1186/s12967-019-2115-9. PMID: 31711520; PMCID: PMC6849246.