2. Cell Cycle/DNA Damage Apoptosis Metabolic Enzyme/Protease Immunology/Inflammation NF-κB
  3. PERK Eukaryotic Initiation Factor (eIF) Bcl-2 Family Apoptosis Reactive Oxygen Species (ROS) STING DNA/RNA Synthesis PD-1/PD-L1
  4. Cytisine-platinum(IV) prodrug-1

Cytisine-Platinum(IV) Prodrug-1 is a Pt(IV) prodrug incorporating the natural compound Cytisine (HY-N0175) with antiproliferative activity against tumor cells. Cytisine-Platinum(IV) Prodrug-1 promotes calcium transfer across the IP3R1-GRP75-VDAC1 axis to drive mitochondrial calcium overload. Cytisine-Platinum(IV) Prodrug-1 initiates unfolded protein response via PERK, eIF2α, ATF4, and CHOP to modulate Bcl-2 and Bax, triggering apoptosis. Cytisine-Platinum(IV) Prodrug-1 induces mitochondrial dysfunction, ROS production, reduced ATP synthesis, DNA damage, and S-phase cell cycle arrest. Cytisine-Platinum(IV) Prodrug-1 activates the cGAS-STING pathway, reduces PD-L1 expression, drives immunogenic cell death. Cytisine-Platinum(IV) Prodrug-1 exhibits high physiological stability, efficient cellular accumulation, and enhanced platinum-DNA binding, and inhibits tumor growth in mouse models with reduced systemic toxicity. Cytisine-Platinum(IV) Prodrug-1 can be used for the research of lung cancer.

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Cytisine-platinum(IV) prodrug-1

Cytisine-platinum(IV) prodrug-1 Chemical Structure

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Cytisine-platinum(IV) prodrug-1 Related Antibodies

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Description

Cytisine-Platinum(IV) Prodrug-1 is a Pt(IV) prodrug incorporating the natural compound Cytisine (HY-N0175) with antiproliferative activity against tumor cells. Cytisine-Platinum(IV) Prodrug-1 promotes calcium transfer across the IP3R1-GRP75-VDAC1 axis to drive mitochondrial calcium overload. Cytisine-Platinum(IV) Prodrug-1 initiates unfolded protein response via PERK, eIF2α, ATF4, and CHOP to modulate Bcl-2 and Bax, triggering apoptosis. Cytisine-Platinum(IV) Prodrug-1 induces mitochondrial dysfunction, ROS production, reduced ATP synthesis, DNA damage, and S-phase cell cycle arrest. Cytisine-Platinum(IV) Prodrug-1 activates the cGAS-STING pathway, reduces PD-L1 expression, drives immunogenic cell death. Cytisine-Platinum(IV) Prodrug-1 exhibits high physiological stability, efficient cellular accumulation, and enhanced platinum-DNA binding, and inhibits tumor growth in mouse models with reduced systemic toxicity. Cytisine-Platinum(IV) Prodrug-1 can be used for the research of lung cancer[1].

IC50 & Target[1]

eIF2

 

Bcl-2

 

Bax

 

In Vitro

Cytisine-Platinum(IV) Prodrug-1 (Compound CP12) (72 h) potently inhibits the viability of H226, SW1990, HepG2, and MDA-MB-231 tumor cells with IC50 values of 0.09, 0.15, 0.21, and 0.61 μM, while showing high selectivity for tumor cells over normal PUMC-HUVEC-T1 cells[1].
Cytisine-Platinum(IV) Prodrug-1 (100 μM; 12-72 h) exhibits high stability in PBS, RPMI-1640 medium, and rat plasma when incubated at 37 °C[1].
Cytisine-Platinum(IV) Prodrug-1 (100 μM; 16 h) undergoes intracellular reductive activation in H226 cells, releasing the cytisine derivative CYT-COOH[1].
Cytisine-Platinum(IV) Prodrug-1 (1 μM; 24 h) potently inhibits colony formation in H226 cells and effectively kills H226 cells[1].
Cytisine-Platinum(IV) Prodrug-1 (1 μM; 24 h) potently inhibits the migration and apoptosis of H226 cells[1].
Cytisine-Platinum(IV) Prodrug-1 (1 μM; 12 h) induces strong S-phase cell cycle arrest in H226 cells, with 62.19% of cells accumulating in S phase, and reduces cyclin D1 expression[1].
Cytisine-Platinum(IV) Prodrug-1 (1 μM; 24 h) induces endoplasmic reticulum stress in H226 cells, activates the IP3R1-GRP75-VDAC1 axis, and causes mitochondrial calcium overload, which contributes to its antitumor activity[1].
Cytisine-Platinum(IV) Prodrug-1 (1 μM; 24 h) induces mitochondrial dysfunction in H226 cells, characterized by reduced ATP production, MMP collapse, increased ROS generation, cytochrome C release, and disrupted mitochondrial morphology[1].
Cytisine-Platinum(IV) Prodrug-1 (1 μM; 24 h) activates the cGAS-STING pathway in H226 cells, upregulating key pathway proteins and promoting IL-6 secretion[1].
Cytisine-Platinum(IV) Prodrug-1 (1 μM; 24 h) potently induces immunogenic cell death in H226 cells, characterized by increased CRT exposure, HMGB1, LDH, and ATP release, and reduced PD-L1 expression[1].

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

Cytisine-platinum(IV) prodrug-1 Related Antibodies

Cell Migration Assay [1]

Cell Line: H226
Concentration: 1 μM
Incubation Time: 24 h
Result: Drastically suppressed H226 cell migration, resulting in a wound healing rate of only 2.44%.

Apoptosis Analysis[1]

Cell Line: H226
Concentration: 1 μM
Incubation Time: 24 h
Result: Induced a high rate of apoptosis in H226 cells, with an apoptosis rate of 80.4%.

Cell Cycle Analysis[1]

Cell Line: H226
Concentration: 1 μM
Incubation Time: 12 h
Result: Resulted in significant S-phase cell cycle arrest in H226 cells, with 62.19% of cells in S phase, and complete blockage of transition from S to G2 phase.
Reduced cyclin D1 protein expression.

Western Blot Analysis[1]

Cell Line: H226
Concentration: 1 μM
Incubation Time: 24 h
Result: Significantly upregulated protein expression of p-PERK, p-eIF2α, ATF4, and CHOP, while downregulating Bcl-2 and upregulating Bax.
Upregulated expression of IP3R1, GRP75, and VDAC1, key components of the ER-mitochondria calcium transfer axis.
Resulted in a significant increase in both cytosolic and mitochondrial Ca2+ levels.
Pretreatment with 2-APB reduced Ca2+ accumulation in the cytosol and mitochondria, and partially reversed CP12-induced cytotoxicity.

Western Blot Analysis[1]

Cell Line: H226
Concentration: 1 μM
Incubation Time: 24 h
Result: Significantly upregulated protein expression of cGAS, p-STING, p-IRF3, and p-TBK1, indicating activation of the cGAS-STING pathway.
Induced the highest level of IL-6 secretion among tested compounds, with levels 2.14-fold higher than those induced by CDDP.

Immunofluorescence[1]

Cell Line: H226
Concentration: 1 μM
Incubation Time: 24 h
Result: Significantly increased CRT surface exposure and HMGB1 release, and reduced PD-L1 protein expression in H226 cells.
In Vivo

Cytisine-Platinum(IV) Prodrug-1 (Compound CP12) (2-4 mg/kg Pt; i.v.; once every 3 days; 6 total doses) potently inhibits H226 lung cancer tumor growth in nude mice, with no significant hepatorenal toxicity and minimal body weight impact[1].
Cytisine-Platinum(IV) Prodrug-1 (2-4 mg/kg Pt; i.v.; once every 3 days; 6 total doses) potently inhibits LLC lung cancer tumor growth in immunocompetent mice, while activating the cGAS-STING pathway, inducing immunogenic cell death, and enhancing cytotoxic T-cell infiltration to remodel the tumor microenvironment[1].

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

Animal Model: BALB/c nude (male, 4-6 weeks old, 18 g, H226 cell-derived xenograft model)[1]
Dosage: 2, 4 mg/kg Pt
Administration: i.v.; once every 3 days; 6 total doses
Result: Achieved a tumor growth inhibition (TGI) rate of 59.3%.
Achieved a tumor growth inhibition (TGI) rate of 72.7%.
Showed no significant body weight loss, with the low-dose group having body weight comparable to the control group, and the high-dose group showing an increasing body weight trend.
Caused no remarkable abnormalities in liver, lung, or kidney tissue.
Achieved significantly higher platinum accumulation in tumor tissue and lower platinum accumulation in renal tissue compared to CDDP (HY-17394).
Induced a concentration-dependent increase in necrotic area in tumor tissue.
Animal Model: C57BL/6 (male, 5 weeks old, 18 g, LLC cell-derived xenograft model)[1]
Dosage: 2, 4 mg/kg Pt
Administration: i.v.; once every 3 days; 6 total doses
Result: Achieved a tumor growth inhibition (TGI) rate of 69.1%.
Achieved a tumor growth inhibition (TGI) rate of 81.1%.
Showed no significant body weight loss.
Potently activated the cGAS-STING pathway in tumor tissue in a dose-dependent manner.
Significantly increased calreticulin (CRT) exposure and high mobility group box 1 (HMGB1) release in tumor tissue.
Substantially increased infiltration of CD3+ and CD8+ T cells in tumors compared to control and CDDP groups.
Molecular Weight

831.74

Formula

C29H51Cl2N5O6Pt
SMILES

[NH3][Pt](Cl)(Cl)([NH3])(OC(CCCC(N1C[C@](C2=CC=CC(N2C[C@@]3(C1)[H])=O)(C3)[H])=O)=O)OC(NCCCCCCCCCCCC)=O
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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Cytisine-platinum(IV) prodrug-1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Cytisine-platinum(IV) prodrug-1PERKEukaryotic Initiation Factor (eIF)Bcl-2 FamilyApoptosisReactive Oxygen Species (ROS)STINGDNA/RNA SynthesisPD-1/PD-L1Protein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinaseStimulator of Interferon GenesTMEM173MITAERISMPYSPD-1/Programmed death-ligand 1mitochondrial calcium overloadATF4eIF2αIP3R1-GRP75-VDAC1 axisH226CHOPlung cancerendoplasmic reticulum stresscGAS-STING-TBK1-IRF3 pathwayInhibitorinhibitorinhibit

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