| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
BRD4 5193 nM (IC50)
UMB298 targets the bromodomains of CBP (CREB-binding protein) and P300, which are histone acetyltransferases involved in transcriptional regulation. It also inhibits BRD4 with an IC50 of 5193 nM. The compound selectively inhibits CBP/P300 bromodomain function. |
|---|---|
| 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].
UMB298 (0.01-10 μM; 50 days) suppresses the proliferation of MOLM13 and MM cells. UMB298 (1-10 μM; 2 hours; MOLM13 cells) decreases H3K27ac levels and induces MYC depletion, which is a marker of CBP inhibition in acute myeloid leukemia. UMB298 downregulates MYC expression. |
| ln Vivo |
In vivo activity data for UMB298 are limited. As a CBP/P300 bromodomain inhibitor, it is expected to have antitumor effects in AML and multiple myeloma models. Further in vivo studies are needed to fully characterize its efficacy and safety profile.
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| Enzyme Assay |
In vitro enzyme assays measure bromodomain inhibition using binding assays or AlphaScreen technology. IC50 values are determined for CBP, P300, and BRD4. Selectivity is confirmed by testing against other bromodomain-containing proteins.
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| 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. Cell-based assays use MOLM13 (AML) and MM (multiple myeloma) cells to measure proliferation inhibition. H3K27ac levels are assessed by Western blot analysis to confirm CBP inhibition. MYC expression is measured to assess the functional consequences of CBP inhibition. |
| Animal Protocol |
In vivo efficacy is evaluated in xenograft models of AML and multiple myeloma. The compound's ability to inhibit tumor growth through CBP/P300 bromodomain inhibition is assessed. Further studies are needed to fully characterize its in vivo antitumor activity.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for UMB298 are limited. As a small molecule bromodomain inhibitor with a molecular weight of 479.01 (C27H31ClN4O2), it may have favorable oral bioavailability. Further pharmacokinetic studies are needed to determine its ADME properties.
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| Toxicity/Toxicokinetics |
Preclinical toxicity data for UMB298 are limited. As a CBP/P300 bromodomain inhibitor, it may have on-target effects related to transcriptional regulation. Standard laboratory safety precautions should be followed. Further toxicological studies are needed for comprehensive safety assessment.
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| References | |
| Additional Infomation |
UMB298 is a potent and selective CBP/P300 bromodomain inhibitor. It suppresses proliferation of AML and multiple myeloma cells, decreases H3K27ac levels, and induces MYC depletion. UMB298 is a valuable research tool for studying CBP/P300 biology and has potential therapeutic applications in hematological malignancies.
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| Molecular Formula |
C27H31CLN4O2
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|---|---|
| Molecular Weight |
479.013645410538
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| Exact Mass |
478.21
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| Elemental Analysis |
C, 67.70; H, 6.52; Cl, 7.40; N, 11.70; O, 6.68
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| CAS # |
2266569-73-5
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| PubChem CID |
137409212
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| Appearance |
White to light yellow solid powder
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| LogP |
7.6
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
34
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| Complexity |
650
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=C(C(=NO1)C)C2=CC3=NC(=C(N3C=C2)NC4CCCCC4)CCC5=CC(=C(C=C5)OC)Cl
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| InChi Key |
NZXSWCLCRDCHGN-UHFFFAOYSA-N
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| 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
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| Chemical Name |
2-(3-chloro-4-methoxyphenethyl)-N-cyclohexyl-7-(3,5-dimethylisoxazol-4-yl)imidazo[1,2-a]pyridin-3-amine
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| Synonyms |
UMB298; UMB-298; UMB 298;
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : 25 mg/mL (52.19 mM)
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|---|---|
| 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.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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