2. Apoptosis Cell Cycle/DNA Damage
  3. Apoptosis Checkpoint Kinase (Chk) CDK DNA/RNA Synthesis Bcl-2 Family Caspase
  4. Apoptosis inducer 49

Apoptosis inducer 49 is a selective apoptosis inducer with high specificity against CCRF-CEM leukemia cells (IC50 = 2.68 μM). Apoptosis inducer 49 enhances RNA synthesis and replication stress, activates the Chk1-p21 axis, leading to S-phase arrest. Apoptosis inducer 49 can inhibit Bcl-2 and activate caspase-3. Apoptosis inducer 49 can be used for the study of Leukemia.

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Apoptosis inducer 49

Apoptosis inducer 49 Chemical Structure

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Apoptosis inducer 49 Related Antibodies

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Description

Apoptosis inducer 49 is a selective apoptosis inducer with high specificity against CCRF-CEM leukemia cells (IC50 = 2.68 μM). Apoptosis inducer 49 enhances RNA synthesis and replication stress, activates the Chk1-p21 axis, leading to S-phase arrest. Apoptosis inducer 49 can inhibit Bcl-2 and activate caspase-3. Apoptosis inducer 49 can be used for the study of Leukemia[1].

In Vitro

Apoptosis inducer 49 (Compound 16j) exhibits potent cytotoxicity against CCRF-CEM cells (IC50 = 2.68 μM), shows no significant activity against other cancer cell lines and non-cancer cell lines (IC50 > 50 μM), and the therapeutic index (TI) is 18.66[1].
Apoptosis inducer 49 (2.68-13.4 μM, 24 h) demonstrates a dose-dependent increase in the proportion of apoptotic cells and induces significant S-phase arrest in CCRF-CEM cells, where at 2.68 μM, early apoptotic (annexin V+/PI-) cells significantly increase concurrently with a rise in S-phase cells and a decrease in G1 and G2/M populations, while at 13.4 μM, late apoptotic (annexin V+/PI+) cells further accumulate and the S-phase arrest effect becomes more pronounced[1].
Apoptosis inducer 49 (2.68-13.4 μM, 24 h) shows dose-dependent inhibition of DNA replication (nearly complete inhibition at 13.4 μM), but RNA synthesis is enhanced, especially at 13.4 μM in CCRF-CEM cells[1].
Apoptosis inducer 49 (2.68-13.4 μM, 24 h) shifts the cell population toward the P3 region (high red/green fluorescence) in CCRF-CEM cells, indicating mitochondrial hyperpolarization (increased ΔΨm) rather than typical apoptosis-associated depolarization[1].
Apoptosis inducer 49 (2.68-13.4 μM, 24 h) induces DNA damage and replication stress, activates the Chk1-p21 axis leading to S-phase arrest, and triggers apoptosis via the mitochondrial pathway (Bcl-2 inhibition and caspase-3 activation) in CCRF-CEM cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis inducer 49 Related Antibodies

Apoptosis Analysis[1]

Cell Line: CCRF-CEM cells
Concentration: 2.68 μM, 13.4 μM
Incubation Time: 24 h
Result: At 2.68 μM, early apoptotic (annexin V+/PI-) cells significantly increased.
At 13.4 μM, late apoptotic (annexin V+/PI+) cells further accumulated.
PI single-positive cells (necrosis markers) were extremely rare.

Western Blot Analysis[1]

Cell Line: CCRF-CEM cells
Concentration: 2.68 μM, 13.4 μM
Incubation Time: 24 h
Result: Caused a moderate increase in Cyclin A expression at both concentrations.
Total Chk1 levels remained stable or slightly elevated at 2.68 μM, while phospho-Chk1 (Ser345), a canonical marker of ATR-mediated replication checkpoint activation, was robustly induced at both 2.68 μM and 13.4 μM.
P21 expression was strongly induced at 2.68 μM.
Induced γH2AX at both concentrations.
Bcl-2 expression was diminished at 13.4 μM.
Caspase-3 was clearly diminished at high concentrations.

Cell Cycle Analysis[1]

Cell Line: CCRF-CEM cells
Concentration: 2.68 μM, 13.4 μM
Incubation Time: 24 h
Result: Caused significant S-phase arrest, at 2.68 μM, the proportion of cells in S phase increased, and the G1 and G2/M populations decreased; the effect was more pronounced at 13.4 μM.
Molecular Weight

575.82

Formula

C36H53N3O3
SMILES

CC1(C)[C@@H](O)CC[C@]2(C)[C@@]3([H])CC[C@]4([H])[C@@]5([H])[C@H](C(C6=CN(CC7=CC=CO7)N=N6)=C)CC[C@@](CO)5CC[C@](C)4[C@@](C)3CC[C@@]12[H]
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Apoptosis inducer 49 Related Classifications

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Keywords:

Apoptosis inducer 49Apoptosis inducer49Apoptosis inducer-49ApoptosisCheckpoint Kinase (Chk)CDKDNA/RNA SynthesisBcl-2 FamilyCaspaseCyclin dependent kinaseLupane triterpenoidsSelective cytotoxicityCCRF-CEM cellsDNA damage responseInhibitorinhibitorinhibit

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