L-Moses HCl | PCAF inhibitor

MedKoo Cat#: 574111 | Name: L-Moses HCl

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Description:

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

L-Moses HCl is an inhibitor of the p300/CBP-associated factor (PCAF) bromodomain. It displaces the PCAF bromodomain from histone H3.3 in a nanoBRET target engagement assay when used at a concentration of 5 μM.

Chemical Structure

L-Moses HCl

CAS#NONE

Theoretical Analysis

MedKoo Cat#: 574111

Name: L-Moses HCl

CAS#: NONE

Chemical Formula: C21H26Cl2N6

Exact Mass: 432.1596

Molecular Weight: 433.38

Elemental Analysis: C, 58.20; H, 6.05; Cl, 16.36; N, 19.39

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 415.00	2 Weeks
10mg	USD 650.00	2 Weeks

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Related CAS #

No Data

Synonym

L-Moses HCl, L-Moses hydrochloride, L-45 HCl

IUPAC/Chemical Name

(1S,2S)-N1,N1-dimethyl-N2-(3-methyl-1,2,4-triazolo[3,4-a]phthalazin-6-yl)-1-phenyl-1,2-propanediamine, dihydrochloride

InChi Key

PCQCTBXCEBIRAC-YRRRDGBXSA-N

InChi Code

InChI=1S/C21H24N6.2ClH/c1-14(19(26(3)4)16-10-6-5-7-11-16)22-20-17-12-8-9-13-18(17)21-24-23-15(2)27(21)25-20;;/h5-14,19H,1-4H3,(H,22,25);2*1H/t14-,19+;;/m0../s1

SMILES Code

CN(C)[C@@H](C1=CC=CC=C1)[C@H](C)NC(C2=CC=CC=C23)=NN4C3=NN=C4C.Cl.Cl

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

>3 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:

L-Moses HCl is an inhibitor of the p300/CBP-associated factor (PCAF) bromodomain.

In vitro activity:

L-45 was shown to disrupt PCAF-Brd histone H3.3 interaction in cells using a nanoBRET assay, and a co-crystal structure of L-45 with the homologous Brd PfGCN5 from Plasmodium falciparum rationalizes the high selectivity for PCAF and GCN5 bromodomains. Reference: Angew Chem Int Ed Engl. 2017 Jan 16;56(3):827-831. https://pubmed.ncbi.nlm.nih.gov/27966810/

In vivo activity:

TBD

	Solvent	mg/mL	mM
Solubility
	DMSO	43.3	100.00
	Water	43.3	100.00

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 433.38 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. Hanquier J, Gimeno T, Jeffers V, Sullivan WJ Jr. Evaluating the GCN5b bromodomain as a novel therapeutic target against the parasite Toxoplasma gondii. Exp Parasitol. 2020 Feb 28;211:107868. doi: 10.1016/j.exppara.2020.107868. Epub ahead of print. PMID: 32119930; PMCID: PMC7483680. 2. Moustakim M, Clark PG, Trulli L, Fuentes de Arriba AL, Ehebauer MT, Chaikuad A, Murphy EJ, Mendez-Johnson J, Daniels D, Hou CD, Lin YH, Walker JR, Hui R, Yang H, Dorrell L, Rogers CM, Monteiro OP, Fedorov O, Huber KV, Knapp S, Heer J, Dixon DJ, Brennan PE. Discovery of a PCAF Bromodomain Chemical Probe. Angew Chem Int Ed Engl. 2017 Jan 16;56(3):827-831. doi: 10.1002/anie.201610816. Epub 2016 Dec 14. PMID: 27966810; PMCID: PMC5412877.

In vitro protocol:

In vivo protocol:

TBD

1. Moustakim, M., Clark, P.G.K., Trulli, L., et al. Discovery of a PCAF Bromodomain Chemical Probe. Angew Chem. Int. Ed. Engl. 56(3), 827-831 (2017).