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.
For research use only. We do not sell to patients.
- Formula: C136H179N31O42S
- Molecular Weight:2952.12
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
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
|
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 |
In Vitro
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.
Chemical Information
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Molecular Weight 2952.12
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Formula 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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Sequence
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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Sequence Shortening
AAQYQDRYYDEFTWKEKDMDYW
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)