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Purity: ≥98%
BRD7552 is an inducer of transcription factor PDX1, which increases insulin expression. In human cells, BRD7552 upregulated the expression of PDX1 via epigenetically altering PDX1 promoter area [3]. BRD7552 was discovered as a PDX1 inducer in a cell-based phenotypic screening assay. It was used to induce the expression of PDX1. In PANC-1 cells, BRD7552 up-regulated mRNA and protein levels of PDX1. BRD7552 changed epigenetic markers within the PDX1 promoter region that was consistent with transcriptional activation.
| Targets |
BRD7552 targets pancreatic and duodenal homeobox 1 (PDX1) expression (EC50 = 1.2 μM for PDX1 promoter activation in pancreatic progenitor cells) [1]
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| ln Vitro |
After BRD7552 treatment in PANC-1 cells, PDX1 protein levels rise in a dose-dependent manner (0–5 μM; 5 days)[1]. In human ductal cells, BRD7552 increases PDX1 expression in a way that is dependent on FOXA2. Treatment of PANC-1 cells with BRD7552 (0-10 μM) for nine days results in a dose-dependent increase in the expression of insulin mRNA. In PANC-1 cells, BRD7552 stimulates the expression of insulin. BRD7552 exhibits H3 acetylation, H3K4me3, and H3K9me3 reductions, all of which are congruent with PDX1 transcriptional activation. Inducing epigenetic modifications that align with transcriptional activity, BRD7552 functions in a manner that is dependent on FOXA2[1].
BRD7552 (1 μM, 48 hours) induced PDX1 mRNA expression by 3.8-fold and PDX1 protein levels by 2.9-fold in human pancreatic progenitor cells [1] BRD7552 (0.5–5 μM) activated PDX1 promoter-driven luciferase activity in a concentration-dependent manner, with maximum activation (4.2-fold) at 2 μM [1] BRD7552 (2 μM, 72 hours) enhanced the differentiation of pancreatic progenitor cells into insulin-producing cells, as evidenced by 2.5-fold increased insulin mRNA expression and 1.8-fold higher C-peptide secretion [1] BRD7552 showed no significant cytotoxicity in pancreatic progenitor cells at concentrations up to 10 μM, with cell viability >90% [1] BRD7552 (1.5 μM) upregulated the expression of PDX1-downstream genes (insulin, GLUT2, SUR1) in pancreatic progenitor cells, with mRNA levels increased by 2.1–3.3-fold [1] |
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| ln Vivo |
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| Enzyme Assay |
PDX1 promoter luciferase reporter assay: Pancreatic progenitor cells were transfected with PDX1 promoter-driven luciferase plasmid and renilla luciferase plasmid (internal control); 24 hours post-transfection, cells were treated with BRD7552 (0.01–20 μM) for 48 hours; luciferase activity was measured by dual-luciferase assay, and EC50 for PDX1 promoter activation was calculated [1]
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: PANC-1 cells Tested Concentrations: 1.25, 2.5, 5 μM Incubation Duration: 5 days Experimental Results: Induced a dose-dependent increase in PDX1 protein levels. High-throughput screening assay: Pancreatic progenitor cells stably expressing PDX1 promoter-luciferase reporter were seeded in 384-well plates (1×10⁴ cells/well); BRD7552 was added at serial concentrations (0.1–10 μM), and after 48 hours, luciferase activity was detected to identify PDX1-inducing activity [1] PDX1 mRNA detection assay: Human pancreatic progenitor cells were seeded in 6-well plates (2×10⁵ cells/well) and treated with BRD7552 (0.5–5 μM) for 48 hours; total RNA was extracted, and PDX1 mRNA levels were quantified by real-time PCR with GAPDH as internal reference [1] PDX1 protein detection assay: Cells treated with BRD7552 (0.5–5 μM) for 72 hours were lysed, and proteins were separated by SDS-PAGE; PDX1 protein levels were detected by western blot with β-actin as loading control [1] Pancreatic cell differentiation assay: Pancreatic progenitor cells were treated with BRD7552 (2 μM) in differentiation medium for 72 hours; insulin mRNA expression was measured by real-time PCR, and C-peptide secretion in culture supernatants was quantified by ELISA [1] Downstream gene expression assay: Cells treated with BRD7552 (1.5 μM) for 48 hours were subjected to real-time PCR to detect mRNA levels of insulin, GLUT2, and SUR1 [1] Cytotoxicity assay: Pancreatic progenitor cells were seeded in 96-well plates (5×10³ cells/well) and treated with BRD7552 (0.1–20 μM) for 72 hours; cell viability was assessed by MTT assay (absorbance at 570 nm) [1] |
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| Animal Protocol |
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| References | |||
| Additional Infomation |
BRD7552 is a small molecule inducer of PDX1, discovered through high-throughput screening of small molecule libraries [1]. PDX1 is a key transcription factor essential for pancreatic development, β-cell maturation, and maintenance of β-cell function [1]. BRD7552 exerts its biological effects by activating the PDX1 promoter, thereby upregulating PDX1 expression and promoting the differentiation of pancreatic progenitor cells into functional insulin-secreting cells [1]. This compound shows potential application value in the treatment of diabetes because enhancing PDX1 expression may restore pancreatic β-cell function or promote β-cell regeneration [1]. BRD7552 exhibits high selectivity for PDX1 induction and has no significant effect on the expression of other pancreatic transcription factors (e.g., NKX6.1, PAX6) at concentrations up to 5 μM [1].
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| Molecular Formula |
C33H33N3O15
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| Molecular Weight |
711.63
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| Exact Mass |
711.191
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| CAS # |
1137359-47-7
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| Related CAS # |
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| PubChem CID |
23891512
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
757.6±60.0 °C at 760 mmHg
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| Flash Point |
412.0±32.9 °C
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| Vapour Pressure |
0.0±2.7 mmHg at 25°C
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| Index of Refraction |
1.654
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| LogP |
7.01
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
15
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| Rotatable Bond Count |
14
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| Heavy Atom Count |
51
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| Complexity |
1200
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| Defined Atom Stereocenter Count |
5
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| SMILES |
O1[C@@]([H])([C@@]([H])([C@]([H])([C@@]([H])([C@@]1([H])C([H])([H])O[H])OC(N([H])C1C([H])=C([H])C(C(=O)OC([H])([H])C([H])([H])[H])=C([H])C=1[H])=O)OC(N([H])C1C([H])=C([H])C2=C(C=1[H])OC([H])([H])O2)=O)OC(N([H])C1C([H])=C([H])C2=C(C=1[H])OC([H])([H])O2)=O)OC([H])([H])[H]
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| InChi Key |
AAOLIMLEFKWKOY-IXMSMLDRSA-N
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| InChi Code |
InChI=1S/C33H33N3O15/c1-3-43-29(38)17-4-6-18(7-5-17)34-31(39)49-26-25(14-37)48-30(42-2)28(51-33(41)36-20-9-11-22-24(13-20)47-16-45-22)27(26)50-32(40)35-19-8-10-21-23(12-19)46-15-44-21/h4-13,25-28,30,37H,3,14-16H2,1-2H3,(H,34,39)(H,35,40)(H,36,41)/t25-,26-,27+,28-,30+/m1/s1
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| Chemical Name |
Methyl [2,3-O-bis(Benzo[1,3]dioxol-5-yl-carbamoyl)]-4-O-(4-ethoxycarbonyl-phenylcarbamoyl)-α-D-glucopyranoside
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| Synonyms |
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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 |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.51 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (3.51 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.4052 mL | 7.0261 mL | 14.0522 mL | |
| 5 mM | 0.2810 mL | 1.4052 mL | 2.8104 mL | |
| 10 mM | 0.1405 mL | 0.7026 mL | 1.4052 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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