AMC-3-221
AMC-3-221 is a cereblon-dependent CDK9 PROTAC degrader with a DC50 of 8 nM (MOLM14 AML cells). AMC-3-221 targets CDK9 with an IC50 of 1.7 nM and a Kd of 4.6 nM. AMC-3-221 decreases MCL-1 and c-MYC protein levels as well as MCL-1, c-MYC, and N-MYC RNA levels. AMC-3-221 induces apoptosis and inhibits proliferation in multiple cancer cell lines. AMC-3-221 exhibits proteasome-dependent CDK9 degradation. AMC-3-221 can be used for research on acute myeloid leukemia (AML).
(Pink: CDK9 Target protein ligand; Blue: Cereblon ligand (HY-W093272); Black: linker).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 3106928-52-0
- 分子式: C35H34Cl2FN9O7
- 分子量:782.60
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
製品説明
IC50 & Target
[1]|
CDK9/cyclinT1 1.7 nM (IC50) |
CDK9 4.6 nM (Kd) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MOLM-14 | IC50 |
45.8 nM
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Antileukemic activity against human MOLM14 AML cells assessed as viability reduction after 48 hrs incubation by alamarBlue assay.
Antileukemic activity against human MOLM14 AML cells assessed as viability reduction after 48 hrs incubation by alamarBlue assay.
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42828372 |
| MV4-11 | IC50 |
62.1 nM
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Antileukemic activity against human MV411 AML cells assessed as viability reduction after 48 hrs incubation by alamarBlue assay.
Antileukemic activity against human MV411 AML cells assessed as viability reduction after 48 hrs incubation by alamarBlue assay.
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42828372 |
| MOLM-14 | DC50 |
8 nM
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Degradation of CDK9 protein in human MOLM14 AML cells incubated 4 hrs by Western blot.
Degradation of CDK9 protein in human MOLM14 AML cells incubated 4 hrs by Western blot.
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42828372 |
体外実験
AMC-3-221 (17 h) inhibits cell-free CDK9/Cyclin T1 kinase activity with an IC50 of 1.7 nM[1].
AMC-3-221 (1 h) binds to CDK9 with a Kd of 4.6 nM and to CDK2 with a Kd of 120 nM, while showing lower affinity for CDK1, CDK4, CDK5, and CDK6[1].
AMC-3-221 (48 h) inhibits MOLM14 and MV411 AML cell viability with IC50 values of 45.8 nM and 62.1 nM, respectively[1].
AMC-3-221 (200 nM; 4 h) selectively reduces CDK9 protein by >95% in MOLM14 AML cells without significantly reducing CDK1, CDK2, CDK4, CDK5, or CDK6[1].
AMC-3-221 (200 nM; 4 h) reduces MCL-1 and MYC protein levels by >75-90% in MOLM14 AML cells without reducing BCL-2 or BCL-xL[1].
AMC-3-221 (1-100 nM; 4 h) degrades CDK9 in MOLM14 AML cells with a DC50 of 8 nM[1].
AMC-3-221 (200 nM; 4 h)-mediated CDK9 degradation in MOLM14 AML cells is proteasome-dependent[1].
AMC-3-221 (200 nM; 18 h) induces apoptosis/death in MOLM14 AML cells, reducing viable cells by approximately 70%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:MOLM14 human AML cells
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Concentration:200 nM
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Incubation Time:4 h
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Result:CDK9 protein was reduced by >95%;
CDK1, CDK2, CDK4, CDK5, and CDK6 were not significantly reduced.\nMCL-1 and MYC protein levels were reduced by >75-90%;
BCL-2 and BCL-xL levels were not reduced.
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Cell Line:MOLM14 human AML cells
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Concentration:1, 2, 5, 10, 20, 50, 100 nM
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Incubation Time:4 h
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Result:DC50 for CDK9 protein level was 8 nM.
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Cell Line:MOLM14 human AML cells
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Concentration:5 μM (MG-132 (HY-13259)); 200 nM (AMC-3-221)
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Incubation Time:4 h (MG-132); 4 h (AMC-3-221)
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Result:Without MG-132 pretreatment, CDK9 protein was reduced by >80%;
with MG-132 pretreatment, CDK9 protein was not reduced.
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Cell Line:MOLM14 human AML cells
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Concentration:200 nM
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Incubation Time:18 h; 3 h (early Annexin V+ cells)
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Result:Viable cells were reduced by ~70%, with corresponding increases in early and late apoptotic cells.
化学情報
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CAS 番号 3106928-52-0
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分子量 782.60
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分子式 C35H34Cl2FN9O7
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SMILES
FC1=CC2=C(C(N(C3C(NC(CC3)=O)=O)C2=O)=O)C=C1N(CC4)CCN4C(CN5CCC(NC(C6=NNC=C6NC(C7=C(Cl)C=CC=C7Cl)=O)=O)CC5)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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Detection of Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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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
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)