GSK2879552 | CAS#1401966-69-5 | LSD1 inhibitor

GSK2879552
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 206158

CAS#: 1401966-69-5

Description: GSK2879552 is an orally available, irreversible, inhibitor of lysine specific demethylase 1 (LSD1), with potential antineoplastic activity. Upon administration, GSK2879552 binds to and inhibits LSD1, a demethylase that suppresses the expression of target genes by converting the dimethylated form of lysine at position 4 of histone H3 (H3K4) to mono- and unmethylated H3K4. LSD1 inhibition enhances H3K4 methylation and increases the expression of tumor-suppressor genes. This may lead to an inhibition of cell growth in LSD1-overexpressing tumor cells. LSD1, overexpressed in certain tumor cells, plays a key role in tumor cell growth and survival.

Chemical Structure

GSK2879552

CAS# 1401966-69-5

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 206158
Name: GSK2879552
CAS#: 1401966-69-5
Chemical Formula: C23H28N2O2
Exact Mass: 364.22
Molecular Weight: 364.489
Elemental Analysis: C, 75.79; H, 7.74; N, 7.69; O, 8.78

Price and Availability

Size	Price	Availability	Quantity
25mg	USD 250
50mg	USD 450
100mg	USD 850
200mg	USD 1450
500mg	USD 2250
1g	USD 3250
2g	USD 5950
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: GSK2879552; GSK-2879552; GSK 2879552.

IUPAC/Chemical Name: 4-((4-((((1R,2S)-2-phenylcyclopropyl)amino)methyl)piperidin-1-yl)methyl)benzoic acid

InChi Key: LRULVYSBRWUVGR-FCHUYYIVSA-N

InChi Code: InChI=1S/C23H28N2O2/c26-23(27)20-8-6-18(7-9-20)16-25-12-10-17(11-13-25)15-24-22-14-21(22)19-4-2-1-3-5-19/h1-9,17,21-22,24H,10-16H2,(H,26,27)/t21-,22+/m0/s1

SMILES Code: O=C(O)C1=CC=C(CN2CCC(CN[C@H]3[C@H](C4=CC=CC=C4)C3)CC2)C=C1

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, not in water

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

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Product Data:

Product Data

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Biological target:	GSK2879552 an orally active, selective and irreversible inhibitor of lysine specific demethylase 1 (LSD1/ KDM1A), with potential antineoplastic activity.
In vitro activity:	The SCLC lines that undergo growth inhibition in response to GSK2879552 exhibit DNA hypomethylation of a signature set of probes suggesting this may be used as a predictive biomarker of activity. Reference: Mol Cell Oncol. 2016 Jan 6;3(2):e1117700. https://pubmed.ncbi.nlm.nih.gov/27308632/
In vivo activity:	The tumors in mice treated with GSK2879552 are not only much smaller but also weigh much lesser (Figures 5C–E). Finally, this study estimated the effect of GSK2879552 in the patient-derived xenograft (PDX) model using metastatic BCa tissues and found that GSK2879552 is capable of inhibiting the growth of PDX significantly (Figures 5F–H). Reference: Front Oncol. 2020 Jul 28;10:1234. https://pubmed.ncbi.nlm.nih.gov/32850370/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMF	1.0	2.74
	DMSO	35.0	96.02
	PBS (pH 7.2)	5.0	13.72

Preparing Stock Solutions

The following data is based on the product molecular weight 364.49 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. Huang M, Chen C, Geng J, Han D, Wang T, Xie T, Wang L, Wang Y, Wang C, Lei Z, Chu X. Targeting KDM1A attenuates Wnt/β-catenin signaling pathway to eliminate sorafenib-resistant stem-like cells in hepatocellular carcinoma. Cancer Lett. 2017 Jul 10;398:12-21. doi: 10.1016/j.canlet.2017.03.038. Epub 2017 Apr 2. PMID: 28377178. 2. Mohammad HP, Kruger RG. Antitumor activity of LSD1 inhibitors in lung cancer. Mol Cell Oncol. 2016 Jan 6;3(2):e1117700. doi: 10.1080/23723556.2015.1117700. PMID: 27308632; PMCID: PMC4905412. 3. Sunami Y, Yokoyama T, Yoshino S, Takahara T, Yamazaki Y, Harada H, Nakamura T. BCL11A promotes myeloid leukemogenesis by repressing PU.1 target genes. Blood Adv. 2022 Mar 22;6(6):1827-1843. doi: 10.1182/bloodadvances.2021004558. PMID: 34714913; PMCID: PMC8941473. 4. Xie Q, Tang T, Pang J, Xu J, Yang X, Wang L, Huang Y, Huang Z, Liu G, Tong D, Zhang Y, Wang L, Zhang D, Lan W, Liu Q, Jiang J. LSD1 Promotes Bladder Cancer Progression by Upregulating LEF1 and Enhancing EMT. Front Oncol. 2020 Jul 28;10:1234. doi: 10.3389/fonc.2020.01234. PMID: 32850370; PMCID: PMC7399223.
In vitro protocol:	1. Huang M, Chen C, Geng J, Han D, Wang T, Xie T, Wang L, Wang Y, Wang C, Lei Z, Chu X. Targeting KDM1A attenuates Wnt/β-catenin signaling pathway to eliminate sorafenib-resistant stem-like cells in hepatocellular carcinoma. Cancer Lett. 2017 Jul 10;398:12-21. doi: 10.1016/j.canlet.2017.03.038. Epub 2017 Apr 2. PMID: 28377178. 2. Mohammad HP, Kruger RG. Antitumor activity of LSD1 inhibitors in lung cancer. Mol Cell Oncol. 2016 Jan 6;3(2):e1117700. doi: 10.1080/23723556.2015.1117700. PMID: 27308632; PMCID: PMC4905412.
In vivo protocol:	1. Sunami Y, Yokoyama T, Yoshino S, Takahara T, Yamazaki Y, Harada H, Nakamura T. BCL11A promotes myeloid leukemogenesis by repressing PU.1 target genes. Blood Adv. 2022 Mar 22;6(6):1827-1843. doi: 10.1182/bloodadvances.2021004558. PMID: 34714913; PMCID: PMC8941473. 2. Xie Q, Tang T, Pang J, Xu J, Yang X, Wang L, Huang Y, Huang Z, Liu G, Tong D, Zhang Y, Wang L, Zhang D, Lan W, Liu Q, Jiang J. LSD1 Promotes Bladder Cancer Progression by Upregulating LEF1 and Enhancing EMT. Front Oncol. 2020 Jul 28;10:1234. doi: 10.3389/fonc.2020.01234. PMID: 32850370; PMCID: PMC7399223.

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