UMB298 is a potent and specific CBP/P300 bromodomain inhibitor.

Physicochemical Properties

Molecular Formula	C27H31CLN4O2
Molecular Weight	479.013645410538
Exact Mass	478.21
Elemental Analysis	C, 67.70; H, 6.52; Cl, 7.40; N, 11.70; O, 6.68
CAS #	2266569-73-5
PubChem CID	137409212
Appearance	White to light yellow solid powder
LogP	7.6
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	5
Rotatable Bond Count	7
Heavy Atom Count	34
Complexity	650
Defined Atom Stereocenter Count	0
InChi Key	NZXSWCLCRDCHGN-UHFFFAOYSA-N
InChi Code	InChI=1S/C27H31ClN4O2/c1-17-26(18(2)34-31-17)20-13-14-32-25(16-20)30-23(27(32)29-21-7-5-4-6-8-21)11-9-19-10-12-24(33-3)22(28)15-19/h10,12-16,21,29H,4-9,11H2,1-3H3
Chemical Name	2-(3-chloro-4-methoxyphenethyl)-N-cyclohexyl-7-(3,5-dimethylisoxazol-4-yl)imidazo[1,2-a]pyridin-3-amine
Synonyms	UMB298; UMB-298; UMB 298;
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

Targets	BRD4 5193 nM (IC50)
ln Vitro	UMB298 (0.01~10 μM; 50 days; MM and MOLM13 cells) suppresses the proliferation of cells[1]. Similar to CBP30, UMB298 (1~10 μM; 2 hours; MOLM13 cells) lowers the H3K27ac level and induces MYC depletion, an indication of CBP inhibition in acute myeloid leukemia[1]. MYC expression is downregulated by UMB298 (3 μM; 2 hours; MOLM13 cells)[1].
Cell Assay	Cell Viability Assay[1] Cell Types: MOLM13 and MM cells Tested Concentrations: 0.01~10 μM Incubation Duration: 50 days Experimental Results: Inhibited cells growth. Western Blot Analysis[1] Cell Types: MOLM13 cells Tested Concentrations: 1~10 μM Incubation Duration: 2 hrs (hours) Experimental Results: decreased the H3K27ac level similar to CBP30 and caused MYC depletion as a signature of CBP inhibition in acute myeloid leukemia. RT-PCR[1] Cell Types: MOLM13 cells Tested Concentrations: 3 μM Incubation Duration: 2 hrs (hours) Experimental Results: Down- regulated MYC expression.
References	[1]. Development of Dimethylisoxazole-Attached Imidazo[1,2-a]pyridines as Potent and Selective CBP/P300 Inhibitors. J Med Chem. 2021;64(9):5787-5801.

Solubility Data

Solubility (In Vitro)

DMSO : 25 mg/mL (52.19 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (5.22 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.0876 mL	10.4382 mL	20.8764 mL
	5 mM	0.4175 mL	2.0876 mL	4.1753 mL
	10 mM	0.2088 mL	1.0438 mL	2.0876 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.