HDAC3-IN-5
HDAC3-IN-5 (9c) is a HDAC3 selective inhibitor, with IC50 values of 4.2 nM, 1629 nM and 298.2 nM for HDAC3, HDAC2, HDAC1, respectively. HDAC3-IN-5 (9c) can effectively induce apoptosisin MV4-11 cells in vitro and reduce the expression of anti-apoptotic proteins, the development of HDAC3 selective inhibitors may serve as a potential lead compound to reverse Venetoclax resistance.
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- CAS No.: 3095232-95-1
- Formule: C28H38N4O
- Masse moléculaire:446.63
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
Description
IC50 & Target
[1]|
HDAC3 4.2 nM (IC50) |
HDAC1 298.2 nM (IC50) |
HDAC2 1629 nM (IC50) |
Cellular Effect
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| JeKo-1 | IC50 |
484 nM
Compound: 9c
|
Antiproliferative activity against human JeKo-1 cells assessed as inhibition of cell growth incubated for 48 hrs by resazurin staining based assay
Antiproliferative activity against human JeKo-1 cells assessed as inhibition of cell growth incubated for 48 hrs by resazurin staining based assay
|
[PMID: 39047608] |
| K562 | IC50 |
383 nM
Compound: 9c
|
Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 48 hrs by resazurin staining based assay
Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 48 hrs by resazurin staining based assay
|
[PMID: 39047608] |
| MV4-11 | IC50 |
315 nM
Compound: 9c
|
Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 48 hrs by resazurin staining based assay
Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 48 hrs by resazurin staining based assay
|
[PMID: 39047608] |
Chemical Information
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CAS No. 3095232-95-1
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Masse moléculaire 446.63
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Formule C28H38N4O
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SMILES
O=C(NNCCC)/C=C/C1=CC=C(CN(CCCC)CCC2=C(C)NC3=C2C=CC=C3)C=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)