DpC

Name: DpC
Brand: MedChemExpress
SKU: HY-114243
Rating: 4.5 (0 reviews)

Cat. No.: HY-114243 Purity: 98.73%: Data Sheet
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DpC is a selective, orally active iron chelator with anticancer activity. DpC acts on signaling pathway-related targets such as JNK, NF-κB, and its activity is competitively inhibited by another iron chelator Dp44mT (HY-18973). By chelating intracellular iron and copper ions in tumor cells to form redox-active complexes, DpC induces oxidative stress, activates the JNK, NF-κB pathways and downregulates IκBα, upregulates the expressions of neuroglobin and cytoglobin, activates caspase 3/9 to induce tumor cell apoptosis. It also overcomes P-glycoprotein-mediated multidrug resistance through a lysosome-targeting mechanism, and exhibits broad-spectrum synergistic effects when combined with various chemotherapeutic agents. DpC inhibits tumor metastasis and increases TNF-α levels in the tumor microenvironment to enhance endogenous immune responses. DpC is applicable to the research of various malignancies including neuroblastoma, pancreatic cancer, prostate cancer, lung cancer, and breast cancer.

For research use only. We do not sell to patients.

DpC Chemical Structure

CAS No. : 1382469-39-7

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	Get quote
200 mg	Get quote

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

Caspase 3

Caspase-9

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	<0.03125 μM Compound: DpC	Antiproliferative activity against human A549 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay	[PMID: 32438199]
A549	IC₅₀	0.004 μM Compound: DpC	Antiproliferative activity at human A549 cells after 72 hrs by MTT assay Antiproliferative activity at human A549 cells after 72 hrs by MTT assay	[PMID: 22861499]
BGC-823	IC₅₀	<0.03125 μM Compound: DpC	Antiproliferative activity against human BGC-823 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human BGC-823 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay	[PMID: 32438199]
Capan-2	IC₅₀	0.02 μM Compound: 11; DPC	Cytotoxicity against human Capan2 cells incubated for 24 hrs by MTT assay Cytotoxicity against human Capan2 cells incubated for 24 hrs by MTT assay	[PMID: 30904782]
CFPAC-1	IC₅₀	0.203 μM Compound: 11; DPC	Cytotoxicity against human CFPAC-1 cells incubated for 24 hrs by MTT assay Cytotoxicity against human CFPAC-1 cells incubated for 24 hrs by MTT assay	[PMID: 30904782]
DMS-53	IC₅₀	0.008 μM Compound: DpC	Antiproliferative activity at human DMS53 cells after 72 hrs by MTT assay Antiproliferative activity at human DMS53 cells after 72 hrs by MTT assay	[PMID: 22861499]
EC9706	IC₅₀	<0.03125 μM Compound: DpC	Antiproliferative activity against human EC9706 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human EC9706 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay	[PMID: 32438199]
GES1	IC₅₀	0.44 μM Compound: DPC	Antiproliferative activity against human GES-1 cells assessed as reduction in cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human GES-1 cells assessed as reduction in cell proliferation incubated for 72 hrs by MTT assay	[PMID: 31614257]
GES1	IC₅₀	0.498 μM Compound: DpC	Cytotoxicity against human GES1 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human GES1 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 32438199]
HGC-27	IC₅₀	0.07 μM Compound: DpC	Antiproliferative activity against human HGC-27 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human HGC-27 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay	[PMID: 32438199]
MCF7	IC₅₀	<0.03125 μM Compound: DpC	Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay	[PMID: 32438199]
MGC-803	IC₅₀	0.166 μM Compound: DpC	Antiproliferative activity against human MGC-803 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human MGC-803 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay	[PMID: 32438199]
MIA PaCa-2	IC₅₀	0.005 μM Compound: 11; DPC	Cytotoxicity against human MIAPaCa2 cells incubated for 24 hrs by MTT assay Cytotoxicity against human MIAPaCa2 cells incubated for 24 hrs by MTT assay	[PMID: 30904782]
MRC5	IC₅₀	>10 μM Compound: DpC	Antiproliferative activity at human MRC5 cells after 72 hrs by MTT assay Antiproliferative activity at human MRC5 cells after 72 hrs by MTT assay	[PMID: 22861499]
PANC-1	IC₅₀	0.03 μM Compound: 11; DPC	Cytotoxicity against human PANC1 cells incubated for 24 hrs by MTT assay Cytotoxicity against human PANC1 cells incubated for 24 hrs by MTT assay	[PMID: 30904782]
PC-3	IC₅₀	0.12 μM Compound: DPC	Antiproliferative activity against human PC3 cells assessed as reduction in cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human PC3 cells assessed as reduction in cell proliferation incubated for 72 hrs by MTT assay	[PMID: 31614257]
PC-3	IC₅₀	0.122 μM Compound: DPC	Antiproliferative activity against human PC-3 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human PC-3 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 33153765]
SGC-7901	IC₅₀	<0.03125 μM Compound: DpC	Antiproliferative activity against human SGC-7901 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human SGC-7901 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay	[PMID: 32438199]
SK-N-MC	IC₅₀	0.013 μM Compound: DpC	Antiproliferative activity at human SK-N-MC cells after 72 hrs by MTT assay Antiproliferative activity at human SK-N-MC cells after 72 hrs by MTT assay	[PMID: 22861499]

In Vitro

DpC (24 h; 72 h) exhibits potent and selective antiproliferative activity against PANC-1, PC3, DMS-53, DU-145 and MDA-MB-231 tumor cells. Meanwhile, it produces synergistic effects in combination with 9 clinical chemotherapeutic agents including Abiraterone (HY-70013), Carboplatin (HY-17393), Cisplatin (HY-17394) and Doxorubicin (HY-15142), but shows antagonistic effects when combined with Dp44mT^[1].
Uptake of ¹⁴C-DpC (25 μM; 2 h) by SK-N-MC neuroepithelioma cells depends on temperature- and energy-dependent regulatory mechanisms, and DpC competes with Dp44mT for the same cellular uptake carrier/receptor^[1].
DpC (25 μM; 24 h) exhibits antiproliferative activity against MSC, H9C2, MIHA, HK2 and SK-N-LP cells, with significantly higher activity in SK-N-LP cells than Dp44mT and L1. It also significantly upregulates the expressions of neuroglobin (Ngb) and cytoglobin (Cygb) in SK-N-LP and HK2 cells, increases the levels of phosphorylated JNK, cleaved caspase 3 and cleaved caspase 9, and decreases the level of IkBα^[2].

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

Cell Viability Assay^[1]

Cell Line:	PANC-1 pancreatic cancer cells, PC3 prostate cancer cells, DMS-53 lung cancer cells, DU-145 prostate cancer cells, and MDA- MB-231 breast cancer cell
Concentration:	0.007-0.096 μM (72 h); 6.50-17.10 μM (24 h)
Incubation Time:	24 h, 72 h
Result:	Showed significant antiproliferative activity against five tumor cell lines, with specific IC₅₀ values (24 h/72 h) for: PANC-1 cells (11.40 μM / 0.096 μM), PC3 cells (17.10 μM / 0.007 μM), DMS-53 cells (6.50 μM / 0.020 μM), DU-145 cells (7.90 μM / 0.007 μM), and MDA-MB-231 cells (9.40 μM/0.008 μM).

Western Blot Analysis^[2]

Cell Line:	SK-N-LP
Concentration:	25 μM
Incubation Time:	24 h
Result:	Significantly increased the expression levels of phosphorylated JNK, neuroglobin (Ngb), cytoglobin (Cygb), and cleaved caspase 3 and 9, while significantly decreasing the expression level of IkBα. The ratio of phosphorylated JNK to total JNK was also significantly elevated, and total JNK levels remained unchanged.

In Vivo

DpC (4 mg/kg; tail vein injection; once daily; 3 weeks) significantly reduces tumor imaging ROI values and tumor volumes, increases the levels of Annexin V (+)/PI (+) cells, caspase 3, neuroglobin, cytoglobin and TNFα, slightly decreases IL-10 levels in tumor tissues, slightly inhibits body weight gain of mice, and does not cause obvious toxicity but induces pulmonary exudative inflammation in an orthotopic SK-N-LP/Luciferase neuroblastoma xenograft model in the left adrenal fat pad of nude mice^[2].

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

Animal Model:	BALB/c nu/nu male nude mice (4 weeks old) with orthotopic SK-N-LP/Luciferase neuroblastoma xenograft in the left adrenal gland fat pad^[2]
Dosage:	4 mg/kg
Administration:	Tail vein injection; once daily; for 3 weeks
Result:	After 3 weeks of daily intravenous administration via tail vein, the tumor imaging ROI value and tumor volume were significantly reduced compared with the vehicle control group. The levels of Annexin V(+)/PI(+) cells, caspase 3, neuroglobin, cytoglobin, and tumor necrosis factor-α (TNFα) in tumor tissues were significantly increased, while interleukin-10 (IL-10) levels were slightly decreased. The body weight gain of mice in the DpC-treated group was slightly but significantly reduced, and no obvious toxicity was observed in major organs such as the spleen, heart, kidney, and brain, but exudative inflammation was induced in the lung tissue.

Molecular Weight

353.48

Formula

C₁₉H₂₃N₅S

CAS No.

1382469-39-7

Appearance

Solid

Color

Light yellow to yellow

SMILES

S=C(N/N=C(C1=NC=CC=C1)\C2=NC=CC=C2)N(C3CCCCC3)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 62.5 mg/mL (176.81 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.8290 mL	14.1451 mL	28.2901 mL
5 mM	0.5658 mL	2.8290 mL	5.6580 mL
10 mM	0.2829 mL	1.4145 mL	2.8290 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.88 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (5.88 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.73%

Select Batch:

Data Sheet (283 KB) SDS (479 KB)

COA (248 KB) HNMR (248 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[1]. Guo ZL, et al. The novel thiosemicarbazone, di-2-pyridylketone 4-cyclohexyl-4-methyl-3-thiosemicarbazone (DpC), inhibits neuroblastoma growth in vitro and in vivo via multiple mechanisms. J Hematol Oncol. 2016 Sep 27;9(1):98. [Content Brief]

[2]. Lin Y, et al. Synthesis and in vivo distribution of 2-deoxy-2-aminodiglucose–prednisolone conjugate (DPC). Chinese Chemical Letters, 2012, 23(5): 557-560.

[3]. Dharmasivam M, et al. The thiosemicarbazone, DpC, broadly synergizes with multiple anti-cancer therapeutics and demonstrates temperature- and energy-dependent uptake by tumor cells. Biochim Biophys Acta Gen Subj. 2022;1866(8):130152. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.8290 mL	14.1451 mL	28.2901 mL	70.7254 mL
	5 mM	0.5658 mL	2.8290 mL	5.6580 mL	14.1451 mL
	10 mM	0.2829 mL	1.4145 mL	2.8290 mL	7.0725 mL
	15 mM	0.1886 mL	0.9430 mL	1.8860 mL	4.7150 mL
	20 mM	0.1415 mL	0.7073 mL	1.4145 mL	3.5363 mL
	25 mM	0.1132 mL	0.5658 mL	1.1316 mL	2.8290 mL
	30 mM	0.0943 mL	0.4715 mL	0.9430 mL	2.3575 mL
	40 mM	0.0707 mL	0.3536 mL	0.7073 mL	1.7681 mL
	50 mM	0.0566 mL	0.2829 mL	0.5658 mL	1.4145 mL
	60 mM	0.0472 mL	0.2358 mL	0.4715 mL	1.1788 mL
	80 mM	0.0354 mL	0.1768 mL	0.3536 mL	0.8841 mL
	100 mM	0.0283 mL	0.1415 mL	0.2829 mL	0.7073 mL

DpC Related Classifications

Help & FAQs

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DpC

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