Shopping Cart
- Remove All
Your shopping cart is currently empty
GNE-272
😃Good
Catalog No. T15400Cas No. 1936428-93-1
GNE-272 is a selective inhibitor of CBP/EP300 (IC50: 0.02, 0.03, and 13 μM for CBP, EP300, and BRD4, respectively) and a selective in vivo probe for CBP/EP300.
GNE-272
😃Good
Catalog No. T15400Cas No. 1936428-93-1
GNE-272 is a selective inhibitor of CBP/EP300 (IC50: 0.02, 0.03, and 13 μM for CBP, EP300, and BRD4, respectively) and a selective in vivo probe for CBP/EP300.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 2 mg | $107 | 6-8 weeks | |
| 25 mg | $728 | 6-8 weeks | |
| 50 mg | $946 | 6-8 weeks | |
| 100 mg | $1,490 | 6-8 weeks |
Bulk & Custom
Add to Cart
Questions
View MoreInhibitors Related to "GNE-272"
Curcumin
Cited
Turmeric yellow, Natural Yellow 3, Indian Saffron, Diferuloylmethane
T1516458-37-7
Curcumin (Natural Yellow 3) is a phenolic natural product, an inhibitor of histone acetyltransferase p300/CREB (IC50=25 μM) with specificity. Curcumin has a wide range of pharmacological activities such as antitumor, anti-inflammatory and antioxidant.
AutophagyEpigenetic Reader DomainFerroptosisHDACHistone AcetyltransferaseInfluenza VirusMitophagyNrf2
- $30
Size
QTY
CitedNaphthol AS-E
nAS-E
T785692-78-4
Naphthol AS-E (nAS-E) is an the KIX-KID interaction and CREB-mediated gene transcription inhibitor.
- $30
Size
QTY
3-methyl-1,2,3,4-tetrahydroquinazolin-2-one
T5000624365-65-9
3-methyl-1,2,3,4-tetrahydroquinazolin-2-one is a inhibitor of BRD4 .
- $33
Size
QTY
(+)-JQ-1
Cited
JQ1
T21101268524-70-4
(+)-JQ-1 (JQ1) is a specific, reversible BET bromine domain inhibitor that targets BRD4 (1/2) with IC50 values of 77/33 nM. (+)-JQ-1 induces cell autophagy and inhibits cell proliferation.
- $30
Size
QTY
CitedABBV-744
ABBV744
T46972138861-99-9In house
ABBV-744 is a BDII-selective BET bromodomain inhibitor that inhibits BRD2/3/4. It is used in the research on inflammatory diseases, cancer, and AIDS.
- $39
Size
QTY
Bisdemethoxycurcumin
Didemethoxycurcumin, Curcumin III
TL000724939-16-0
Bisdemethoxycurcumin (Curcumin III) is a natural demethoxy derivative of curcumin. It is a potent activator of macrophage phagocytosis, interacting with 1α, 25-dihydroxy vitamin D3 to stimulate amyloid-β clearance by macrophages (optimal stimulation at 100 nM BDMC) [1]. More stable than curcumin in physiological media, BDMC suppresses proliferation of cancer cells [2]. It down-regulates the transcriptional coactivator p300, suppressing the Wnt/β-catenin pathway, and inhibits LPS induction of iNOS expression [3].
- $31
Size
QTY
dBET6 Cited
T51301950634-92-0
dBET6 is a selective and cell-permeable degrader of BET based on PROTAC (IC50: 14 nM). It has antitumor activity.
- $48
Size
QTY
CitedCeMMEC1
T4345440662-09-9In house
CeMMEC1 is an inhibitor of BRD4, and also has a great affinity for TAF1(IC50=0.9 μM).
- $30
Size
QTY
J-147 Cited
J147
T19931146963-51-0
J-147 is an experimental drug with reported effects against both Alzheimer's disease and ageing in mouse models of accelerated aging. It is a curcumin derivative and a potent neurogenic and neuroprotective drug candidate initially developed for the treatment of neurodegenerative conditions associated with aging that impacts many pathways implicated in the pathogenesis of diabetic neuropathy.
- $40
Size
QTY
CitedPiflufolastat
DCFPYL
T312241423758-00-2In house
Piflufolastat (DCFPYL) is a PET imaging agent for prostate cancer PSMA. It is a fluorinated prostate-specific membrane antigen (PSMA) preparation. Piflufolastat can be used to prepare piflufolastat F 18 (DCFPyL F-18).
- $52
Size
QTY
Anacardic Acid Cited
Hydroginkgolic acid, 6-pentadecylsalicylic Acid
T638916611-84-0
Anacardic Acid (6-pentadecylsalicylic Acid) is an effective inhibitor of p300 and p300/CBP-associated factor histone acetyltranferases. It also has antimicrobial activity, antibacterial activity, and inhibits prostaglandin synthase, lipoxygenase, and tyrosinase.
- $45
Size
QTY
CitedGSK1379725A
T154241802251-00-8
GSK1379725A is a selective BPTF ligand [Kd = 2.8 μM].
- $67
Size
QTY
Contact us for more batch information
Resource Download
Product Introduction
Bioactivity
Chemical Properties
| Description | GNE-272 is a selective inhibitor of CBP/EP300 (IC50: 0.02, 0.03, and 13 μM for CBP, EP300, and BRD4, respectively) and a selective in vivo probe for CBP/EP300. |
| Targets&IC50 | BRD4:13 μM, EP300:0.03 μM, CBP:0.02 μM |
| In vitro | GNE-272 does not inhibit any target at >30% when tested at 10 μM in 35 kinase panel and 42 receptors off-target screening panel. GNE-272 does not inhibit (>10 μM, top concentration) several cytochrome P450s (3A4, 1A2, 2C9, 2C19, 2D6). GNE-272 is exquisitely selective for CBP/ EP300 and remarkably selective (650-fold) over BRD4. The compound has good potency in the BRET cellular assay. GNE-272 is shown to inhibit the expression of MYC10 (MV4?11 cell line) (EC50: 0.91 μM) and a good correlation between the BRET and MYC cellular assays is observed. |
| In vivo | GNE-272 displays a marked antiproliferative effect in hematologic cancer cell lines. Which modulates MYC expression in vivo that corresponds with antitumor activity in an AML tumor model. GNE-272 shows low clearance following a 1 mg/ kg intravenous dose in a mouse PK experiment and good oral bioavailability when dosed at 100 mg/kg, reaching an unbound Cmax of 26 μM. |
| Molecular Weight | 424.47 |
| Formula | C22H25FN6O2 |
| Cas No. | 1936428-93-1 |
| Relative Density. | 1.43 g/cm3 (Predicted) |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 100 mg/mL (235.59 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
| ||||||||||||||||||||||||||||||||||||
Calculator
In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
Preview
Related Tags: buy GNE-272 | purchase GNE-272 | GNE-272 cost | order GNE-272 | GNE-272 chemical structure | GNE-272 in vivo | GNE-272 in vitro | GNE-272 formula | GNE-272 molecular weight
- TOP
Feedback
Hello! How can I help you today? 
Copyright © 2015-2024 TargetMol Chemicals Inc. All Rights Reserved.