CDR3a23
CDR3a23 is a CD38 inhibitor and apoptosis inducer (human Kd = 630 nM) that binds to CD38 epitope 2 to block its function, induces apoptosis and G1 phase cell cycle arrest, thereby inhibiting cell growth. CDR3a23 can be used in research on hematological malignancies.
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- 分子式: C136H179N31O42S
- 分子量:2952.12
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
IC50 & Target
[1]|
CD38 630 nM (Kd) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HL-60 | IC50 |
540 nM
|
Antiproliferative activity against human HL-60 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay.
Antiproliferative activity against human HL-60 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay.
|
40652724 |
| HL-60 | IC50 |
390 nM
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Antiproliferative activity against human HL-60 cells in combination with 1 μM ATRA assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay.
Antiproliferative activity against human HL-60 cells in combination with 1 μM ATRA assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay.
|
40652724 |
体外実験
CDR3a23 (L-pep) (40-800 nM; 4 h) specifically binds to CD38 on the surface of HL-60 cells, with a binding affinity higher than that of cyclic C-pep[1].
CDR3a23 (L-pep) (100-2000 nM; 4 h) binds to CD38 on HL-60 cells with a Kd of 630 nM[1].
CDR3a23 (L-pep) (800 nM; 3 days) exhibits a time-dependent antiproliferative effect on HL-60 cells, but not on SH-SY5Y cells[1].
CDR3a23 (L-pep) (100-1000 nM; 48 h) inhibits HL-60 cell proliferation with an IC50 of 540 nM, which decreases to 390 nM when combined with 1 μM Retinoic acid (ATRA) (HY-14649), while showing no effect on SH-SY5Y cells[1].
CDR3a23 (L-pep) (540 nM; 48 h) induces 47.5% total apoptosis in HL-60 cells at its IC50 concentration, and this proportion increases to 72.5% when combined with 1 μM ATRA[1].
CDR3a23 (L-pep) (540 nM; 48 h) induces G1 phase arrest in 52.21% of HL-60 cells, and this proportion increases to 65.9% when combined with 1 μM ATRA[1].
CDR3a23 peptide (100 ns) stably binds to the active site of human CD38 with a binding energy of -10.2 kcal/mol[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HL-60; SH-SY5Y
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Concentration:800 nM (L-pep)
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Incubation Time:3 days
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Result:Exhibited a substantial and time-dependent anti-proliferative impact on HL-60 cells after 24 h.
Greatly suppressed the proliferation of HL-60 cells in combination with 1 μM ATRA.
Did not affect the population of SH-SY5Y cells even after 72 h.
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Cell Line:HL-60; SH-SY5Y
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Concentration:100, 300, 700, 1000 nM (L-pep)
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Incubation Time:48 h
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Result:Inhibited HL-60 cell proliferation with an IC50 of 540 nM.
Decreased IC50 to 390 nM when combined with 1 μM ATRA.
Had no effect on SH-SY5Y cells.
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Cell Line:HL-60
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Concentration:540 nM (L-pep)
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Incubation Time:48 h
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Result:Induced total apoptosis in 47.5% of HL-60 cells.
Increased total apoptosis to 72.5% when combined with 1 μM ATRA.
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Cell Line:HL-60
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Concentration:540 nM (L-pep)
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Incubation Time:48 h
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Result:Induced G1 phase arrest in 52.21% of HL-60 cells.
Increased G1 phase arrest to 65.9% when combined with 1 μM ATRA.
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- Somatic Cell Culture
- Protocol for Cell Cycle
- CCK-8/WST-8 Cell Proliferation Assay
- Cell Counting-Based Growth Curve Assay
- Cell Viability Determination by MTT Colorimetric Assay
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Protocol for Cell Counting and Cell Density Analysis
- Apoptosis Solutions
- MTT Cell Proliferation Assay
化学情報
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分子量 2952.12
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分子式 C136H179N31O42S
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SMILES
O=C(N[C@@H](C)C(N[C@@H](CCC(N)=O)C(N[C@@H](CC1=CC=C(C=C1)O)C(N[C@@H](CCC(N)=O)C(N[C@@H](CC(O)=O)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CC2=CC=C(C=C2)O)C(N[C@@H](CC3=CC=C(C=C3)O)C(N[C@@H](CC(O)=O)C(N[C@@H](CCC(O)=O)C(N[C@@H](CC4=CC=CC=C4)C(N[C@@H]([C@H](O)C)C(N[C@@H](CC5=CNC6=CC=CC=C56)C(N[C@@H](CCCCN)C(N[C@@H](CCC(O)=O)C(N[C@@H](CCCCN)C(N[C@@H](CC(O)=O)C(N[C@@H](CCSC)C(N[C@@H](CC(O)=O)C(N[C@@H](CC7=CC=C(C=C7)O)C(N[C@@H](CC8=CNC9=CC=CC=C89)C(O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)[C@H](C)N
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配列
Ala-Ala-Gln-Tyr-Gln-Asp-Arg-Tyr-Tyr-Asp-Glu-Phe-Thr-Trp-Lys-Glu-Lys-Asp-Met-Asp-Tyr-Trp
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シーケンスの短縮
AAQYQDRYYDEFTWKEKDMDYW
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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.
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)