Cat. No.: HY-W683756

Copy Link Print Information

Boldine hydrochloride

Name: Boldine hydrochloride
Brand: MedChemExpress
SKU: HY-W683756
Availability: PreOrder

1 Cited Publications

Customer Review

Based on 1 publication(s) in Google Scholar

Boldine hydrochloride is an aporphine alkaloid telomerase (telomerase) inhibitor (IC₅₀ of 0.17 μM for TERT) and a pannexin/connexin hemichannel blocker, with oral activity and blood-brain barrier permeability. Boldine hydrochloride inhibits telomerase activity through direct interaction with the telomerase ribonucleoprotein and non-competitive binding near the TERT active site, and downregulates hTERT mRNA while shifting alternative splicing toward non-functional transcripts. Boldine hydrochloride blocks Panx1, Cx43, Cx26, and Cx30 hemichannels as well as P2X7 receptor-mediated calcium influx. Boldine hydrochloride exhibits antioxidant, anti-inflammatory, antiproliferative, and cytotoxic activities by scavenging ROS, inhibiting NFκB, dephosphorylating SGK1, and reducing TNF-alpha levels. Boldine hydrochloride can be used in research on breast cancer, Alzheimer's disease, glioblastoma, diabetes, and spinal cord injury.

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

CAS No.: 16625-69-7
Formula: C₁₉H₂₂ClNO₄
Molecular Weight:363.84

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Boldine hydrochloride Chemical Structure

CAS No.: 16625-69-7

Size

Price

Stock

Quantity

Amount: USD 0.00

* Please select Quantity before adding items.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

All P2X Receptor Isoforms :

All Calcium Channel Isoforms :

All NF-κB Isoforms :

All SGK Isoforms :

All TNF Receptor Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC50	110 μM	Cytotoxicity against human HEK293 embryonic kidney cells assessed as reduction in cell viability after 48 hrs treatment by MTT assay. Cytotoxicity against human HEK293 embryonic kidney cells assessed as reduction in cell viability after 48 hrs treatment by MTT assay.	25746354
MDA-MB-231	IC50	150 μM	Cytotoxicity against human MDA-MB-231 breast cancer cells assessed as reduction in cell viability after 48 hrs treatment by MTT assay. Cytotoxicity against human MDA-MB-231 breast cancer cells assessed as reduction in cell viability after 48 hrs treatment by MTT assay.	25746354
MCF7	IC50	160 μM	Cytotoxicity against human MCF-7 breast cancer cells assessed as reduction in cell viability after 48 hrs treatment by MTT assay. Cytotoxicity against human MCF-7 breast cancer cells assessed as reduction in cell viability after 48 hrs treatment by MTT assay.	25746354
HFF	IC50	280 μM	Cytotoxicity against human foreskin fibroblasts (HFF) assessed as reduction in cell viability after 48 hrs treatment by MTT assay. Cytotoxicity against human foreskin fibroblasts (HFF) assessed as reduction in cell viability after 48 hrs treatment by MTT assay.	25746354
MCF7	IC50	60 μM	Inhibition of telomerase activity in human MCF-7 breast cancer cell lysates incubated for 48 hrs by SYBR Green q-TRAP assay. Inhibition of telomerase activity in human MCF-7 breast cancer cell lysates incubated for 48 hrs by SYBR Green q-TRAP assay.	25746354
MDA-MB-231	IC50	29.1 μM	Inhibition of telomerase activity in human MDA-MB-231 breast cancer cell lysates incubated for 48 hrs by SYBR Green q-TRAP assay. Inhibition of telomerase activity in human MDA-MB-231 breast cancer cell lysates incubated for 48 hrs by SYBR Green q-TRAP assay.	25746354
HEK293	IC50	38.8 μM	Inhibition of telomerase activity in human HEK293 embryonic kidney cell lysates incubated for 48 hrs by SYBR Green q-TRAP assay. Inhibition of telomerase activity in human HEK293 embryonic kidney cell lysates incubated for 48 hrs by SYBR Green q-TRAP assay.	25746354
U-87MG ATCC	IC50	213.8 μM	Inhibition of cell growth in human U87-MG glioblastoma cells assessed after 72 hrs of treatment by MTT assay. Inhibition of cell growth in human U87-MG glioblastoma cells assessed after 72 hrs of treatment by MTT assay.	37655012
MCF7	LD₅₀	160 μM	Cytotoxicity against human MCF7 breast cancer cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay. Cytotoxicity against human MCF7 breast cancer cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay.	29671783
MDA-MB-231	LD₅₀	150 μM	Cytotoxicity against human MDA-MB-231 breast cancer cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay. Cytotoxicity against human MDA-MB-231 breast cancer cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay.	29671783

In Vitro

Anti-cancerInnate ImmunityOxidative StressOthers

Anti-cancer

Boldine (48 h) hydrochloride exhibits dose- and time-dependent cytotoxicity in HEK293, MDA-MB-231, and MCF-7 cells, with IC₅₀ values of 110 μM, 150 μM, and 160 μM, respectively, while showing less toxicity to normal HFF cells^[1].
Boldine (0-300 μM; 72 h) hydrochloride inhibits the growth of primary human GBM59, GBM96, and U87-MG glioblastoma cells in a concentration-dependent manner, with IC₅₀ values of 68.6 μM, 141.7 μM, and 213.8 μM, respectively^[4].
Boldine (50-300 μM; 15 min) hydrochloride inhibits hemichannel activity in patient-derived GBM59, GBM96, and U87-MG glioblastoma cells^[4].

Innate Immunity

Boldine (10-100 μM; 1 h) hydrochloride prevents LPS (HY-D1056)-induced activation of SGK1 and NFκB in cardiac fibroblasts isolated from neonatal Sprague-Dawley rats^[2].
Boldine (100 μM; 1 h) hydrochloride prevents inflammatory responses induced by LPS, IFN-γ, and conditioned medium in neonatal Sprague-Dawley rat cardiac fibroblasts^[2].

Innate Immunity

Oxidative Stress

Boldine (100 μM; 1 h) hydrochloride prevents LPS-induced oxidative stress in cardiac fibroblasts isolated from neonatal Sprague-Dawley rats^[2].

Oxidative Stress

Boldine hydrochloride directly scavenges superoxide anions and highly reactive hydroxyl radicals^[6].
Boldine (1-100 μM; 1 h (STZ); 30 min (iron/ascorbate)) hydrochloride attenuates lipid peroxidation, protein oxidation, and thiol oxidation induced by STZ (HY-13753) and iron/ascorbate in rat pancreatic homogenates in a dose-dependent manner^[6].

Others

Boldine (0-160 μM; 48 h) hydrochloride significantly inhibits telomerase activity in MCF-7, MDA-MB-231, and HEK293 cells in a dose-dependent manner, with IC₅₀ values of 60 μM, 29.1 μM, and 38.8 μM, respectively^[1].
Boldine (0-160 μM; 48 h) hydrochloride decreases hTERT mRNA levels in MCF-7 cells in a dose-dependent manner^[1].
Boldine (0-160 μM; 48 h) hydrochloride stimulates nonfunctional splice variants of hTERT, and in MCF-7 cells, the -b variant is the only detectable transcript at 160 μM^[1].
Boldine (100-500 μM; 5 min) hydrochloride inhibits hemichannel activity in LPS-treated cultured mouse cortical astrocytes^[3].
Boldine (100 μM) hydrochloride inhibits Panx1 hemichannels in HeLa-Panx1-YPF cells^[3].
Boldine (50 μM; 15 min) hydrochloride inhibits hemichannel activity in rat SVZ neurosphere-derived NPCs^[4].
Boldine (50-100 μM; 72 h) hydrochloride decreases the diameter of rat SVZ neurosphere-derived NPCs and disrupts the integrity of neurospheres^[4].
Boldine hydrochloride (50 μM; 72 h) reduces the proliferation of NPCs derived from rat SVZ neurospheres, as evidenced by decreased BrdU incorporation^[4].
Boldine (50 μM) hydrochloride blocks Cx26 and Cx30 hemichannels and blocks P2X7R in transfected HeLa cells^[8].

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

Real Time qPCR^[1]

Cell Line:

MCF-7
Concentration:

0, 10, 100, 160 μM
Incubation Time:

48 h
Result:

Caused a dose-dependent repression of transcripts of the hTERT gene.

RT-PCR^[1]

Cell Line:

MCF-7
Concentration:

0, 10, 100, 160 μM
Incubation Time:

48 h
Result:

Decreased the full-length variant while the three shorter transcripts were still visible.
At 10 μM, the full-length transcript exhibited a marked decrease while all non-functional variants remained unchanged.
At 160 μM, the -b spliced form was the only detectable variant.

Western Blot Analysis^[2]

Cell Line:

Cardiac fibroblasts (CF) isolated from neonatal Sprague-Dawley rats
Concentration:

10, 50, 100 μM (NFκB phosphorylation); 100 μM (NFκB nuclear localization, SGK1/NDRG1 phosphorylation, SGK1 mRNA)
Incubation Time:

1 h pretreatment followed by 1 μg/mL LPS for 6 h (NFκB phosphorylation, NFκB nuclear localization, SGK1/NDRG1 phosphorylation); 1 h pretreatment followed by 1 μg/mL LPS for 8 h (SGK1 mRNA)
Result:

Prevented NFκB phosphorylation induced by LPS at 100 μM.
Reduced NFκB nuclear localization induced by LPS at 100 μM.
Inhibited LPS-induced activation of SGK1 at 100 μM, evidenced by reduced phosphorylation of SGK1 and its downstream target NDRG after 6 h of LPS treatment.
Decreased SGK1 mRNA expression after 8 h of LPS treatment at 100 μM.

Real Time qPCR^[2]

Cell Line:

Cardiac fibroblasts (CF) isolated from neonatal Sprague-Dawley rats and monocytes derived from rat spleen (SMC)
Concentration:

100 μM (boldine); 1 μg/mL (LPS); 10 ng/mL (IFN-γ); conditioned medium (CM)
Incubation Time:

1 h pretreatment (boldine); 6 h (LPS for protein); 24 h (LPS for adhesion); 4 h (co-incubation with SMC)
Result:

Prevented the LPS-induced increase in pro-inflammatory cytokines IL-1β and TNF-α mRNA expression at 100 μM.
Inhibited the upregulation of ICAM1 and VCAM1 at both protein and mRNA levels at 100 μM.
Reduced monocyte adhesion on LPS-stimulated CFs at 100 μM.
Blocked the increase in ICAM1 and VCAM1 protein levels induced by IFN-γ and CM at 100 μM.
Reduced monocyte adhesion to CFs stimulated by IFN-γ and CM at 100 μM.

Cell Proliferation Assay^[4]

Cell Line:

Rat subventricular zone (SVZ) neural progenitor cells (NPCs)
Concentration:

50 μM
Incubation Time:

72 h
Result:

Reduced BrdU incorporation from 29.3% to 12.7%.

In Vivo

Aβ/Tau/α-Synuclein AggregationGlutamate Release or ReceptorsOxidative StressOthers

Aβ/Tau/α-Synuclein Aggregation

Glutamate Release or Receptors

Boldine (30 mg/kg; p.o.; in drinking water; 12 weeks) hydrochloride prevents glial hemichannel activation, reduces intracellular Ca²⁺ signaling and ATP/glutamate release, and attenuates neuronal damage in APP/PS1 mice without affecting gap junction communication^[3].

Oxidative Stress

Boldine (100 mg/kg; p.o.; daily; 8 weeks) hydrochloride attenuates the development of STZ-induced diabetes in rats by preventing the increase in blood glucose levels, reducing body weight loss, and alleviating oxidative mitochondrial damage in multiple organs^[6].

Others

Boldine (2.5-40 mg/kg; i.p.) hydrochloride significantly inhibits Apomorphine (HY-12723)-induced yawning and penile erection in rats, with an inhibition rate exceeding 50%^[7].
Boldine (50 mg/kg; p.o.; daily; starting from 3 dpi) hydrochloride, administered starting 3 days after contusive SCI, significantly improves motor function, preserves white matter, and reduces glial reactivity in mice^[8].

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

Animal Model:

Sprague-Dawley rats (male, 250-260 g, streptozotocin-induced diabetes)^[6]
Dosage:

100 mg/kg
Administration:

p.o.; daily; 8 weeks
Result:

Attenuated the development of hyperglycemia and weight loss induced by STZ injection.
Reduced plasma glucose levels to 330.6 mg/dl at 4 weeks and 311.4 mg/dl at 8 weeks, compared to 505.2 mg/dl and 538.4 mg/dl in the STZ group.
Attenuated STZ-induced weight loss, with body weight at 8 weeks of 298 g versus 221 g in the STZ group.
Significantly lowered MDA levels in pancreas and liver mitochondria.
Significantly lowered carbonyl contents in pancreas and kidney mitochondria.
Decreased increased MnSOD activities in the pancreas and kidney.
Restored altered GSH-Px enzyme activities in the liver and pancreas.

Animal Model:

Wistar (Charles River, France; male; 220 ± 40 g)^[7]
Dosage:

2.5 mg/kg; 10 mg/kg; 20 mg/kg; 40 mg/kg
Administration:

i.p.; single dose
Result:

Inhibited Apomorphine-induced yawning by more than 50% at 40 mg/kg.
Inhibited Apomorphine-induced penile erections by more than 50% at 40 mg/kg.

Animal Model:

C57Bl6 (male and female, 4 months of age)^[8]
Dosage:

50 mg/kg
Administration:

p.o.; daily; starting at 3 dpi
Result:

Improved locomotor function as assessed by BMS scores in males at 7 dpi (3.41 vs. 2.29), 14 dpi (6.56 vs. 4.61), 21 dpi (7.44 vs. 5.57), and 28 dpi (7.94 vs. 6.11).
Improved locomotor function as assessed by BMS scores in females at 14 dpi (4.84 vs. 3.53), 21 dpi (5.89 vs. 4.88), and 28 dpi (6.46 vs. 5.00).
Showed a lower percentage of foot placement errors in the LRWT at 14 dpi (14.7% vs. 37.4% for males; 21.6% vs. 38.0% for females), 21 dpi (12.0% vs. 30.2% for males; 16.0% vs. 30.1% for females), and 28 dpi (8.9% vs. 23.3% for males; 11.2% vs. 22.0% for females).
Significantly increased spared white matter at 28 dpi and reduced lesion volume.
Reduced immunofluorescence for GFAP and Iba1 while increasing GAP43 fluorescence in sections rostral to the injury site at 14 dpi.
Reduced mRNA levels of Ccl2, IL-6, S100a, Cd68, Iba1, Gfap, and Mmp9, and increased mRNA levels of Snap25 and Gap43 at 14 dpi.
Showed significantly lower levels of Gfap and S100a8 mRNA in RNAscope in-situ hybridization at 14 dpi.
Identified 426 upregulated and 913 downregulated genes in the spinal cord segment caudal to the lesion at 14 dpi.

Related Protocols :

Chemical Information

CAS No. 16625-69-7
Molecular Weight 363.84
Formula C₁₉H₂₂ClNO₄
SMILES

OC1=C(OC)C2=C3C(CCN(C)[C@@]3([H])CC4=CC(O)=C(OC)C=C24)=C1.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (1)

All

Sort by:

Journal Impact Factor

Phytother Res

Total glucosides of white paeony capsule alleviate articular cartilage degeneration and aberrant subchondral bone remodeling in knee osteoarthritis. [Abstract]

2025 Apr;39(4):1758-1775. PMID: 38649260

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Kazemi Noureini S, et al. Boldine, a natural aporphine alkaloid, inhibits telomerase at non-toxic concentrations. Chemico-biological interactions. 2015 Apr 25;231:27-34.

[2]. Catalán M, et al. Boldine prevents the inflammatory response of cardiac fibroblasts induced by SGK1-NFκB signaling pathway activation. Cellular signalling. 2024 Aug;120:111241. [Content Brief]

[3]. Yi C, et al. Inhibition of glial hemichannels by boldine treatment reduces neuronal suffering in a murine model of Alzheimer's disease. Glia. 2017 Oct;65(10):1607-1625. [Content Brief]

[4]. Jiménez-Madrona E, et al. Antiproliferative effect of boldine on neural progenitor cells and on glioblastoma cells. Frontiers in neuroscience. 2023;17:1211467.

[5]. Kazemi Noureini S, et al. Telomerase Inhibition by a New Synthetic Derivative of the Aporphine Alkaloid Boldine. International journal of molecular sciences. 2018 Apr 19;19(4):1239.

[6]. Jang YY, et al. Protective effect of boldine on oxidative mitochondrial damage in streptozotocin-induced diabetic rats. Pharmacological research. 2000 Oct;42(4):361-71.

[7]. Asencio M, et al. Biochemical and behavioral effects of boldine and glaucine on dopamine systems. Pharmacology, biochemistry, and behavior. 1999 Jan;62(1):7-13.

[8]. Toro CA, et al. Boldine modulates glial transcription and functional recovery in a murine model of contusion spinal cord injury. Frontiers in cellular neuroscience. 2023;17:1163436.

Calculators

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Boldine hydrochloride

1 Cited Publications

100 mg Get Quote

Subscribe to the

MedChemExpress

Newsletter

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent:

Product Name:
CAS No.:
Species:
Purity:
Quantity:

Boldine hydrochloride

Publications Citing Use of MedChemExpress (MCE) Boldine hydrochloride

All P2X Receptor Isoforms

All Calcium Channel Isoforms

All NF-κB Isoforms

All SGK Isoforms

All TNF Receptor Isoforms