2. Protein Tyrosine Kinase/RTK Epigenetics
  3. Anaplastic lymphoma kinase (ALK) METTL3
  4. Humantenine

Humantenine is a highly toxic indole alkaloid from Gelsemium elegans (Gardn. & Champ.) Benth. that binds to RNA m6A modification regulatory proteins (ALKBH5, METTL). Humantenine stably binds via hydrogen bonding and hydrophobic interactions and disrupts the m6A methylation level of target genes, thereby impairing the expression of intestinal epithelial cell tight junction and cytoskeleton-related genes, causing intestinal barrier dysfunction and significant intestinal cytotoxicity. The intraperitoneal injection LD50 values of Humantenine are <1 mg/kg in mice, 1.2 mg/kg in male rats and 1.5 mg/kg in female rats, respectively. Species differences exist in the metabolism of Humantenine in human, porcine, goat and rat liver microsomes, and demethylation, dehydrogenation and oxidation occur in liver microsomes.

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

Humantenine

Humantenine Chemical Structure

CAS No. : 82375-29-9

Size Price Stock Quantity
1 mg In-stock
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg   Get quote  
100 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Humantenine Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Humantenine is a highly toxic indole alkaloid from Gelsemium elegans (Gardn. & Champ.) Benth. that binds to RNA m6A modification regulatory proteins (ALKBH5, METTL). Humantenine stably binds via hydrogen bonding and hydrophobic interactions and disrupts the m6A methylation level of target genes, thereby impairing the expression of intestinal epithelial cell tight junction and cytoskeleton-related genes, causing intestinal barrier dysfunction and significant intestinal cytotoxicity. The intraperitoneal injection LD50 values of Humantenine are <1 mg/kg in mice, 1.2 mg/kg in male rats and 1.5 mg/kg in female rats, respectively. Species differences exist in the metabolism of Humantenine in human, porcine, goat and rat liver microsomes, and demethylation, dehydrogenation and oxidation occur in liver microsomes[1][2][3][4][5].

Cellular Effect
Cell Line Type Value Description References
A-431 EC50
> 100 μM
Compound: humantenine
Cytotoxicity against human A431 cells after 48 hrs by trypan blue test
Cytotoxicity against human A431 cells after 48 hrs by trypan blue test
[PMID: 16643063]
In Vitro

Humantenine (400 μM; 48 h) induces concurrent alterations in m6A modification and expression of mRNA for 1401 genes in the human colon cancer cell line HCT116, leading to the enrichment of KEGG and GO annotation terms related to actin cytoskeleton, tight junctions and adherens junctions, differential expression of 11 RNA m6A methylation regulators, and dysregulated m6A methylation levels of target genes[1].
Humantenine (10 mM; 1 h) undergoes metabolism via 5 pathways in human liver microsomes, with demethylation as the major metabolic pathway, producing 9 distinct metabolites with specific semi-quantitative peak intensities[2].

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

Humantenine Related Antibodies

Cell Viability Assay[1]

Cell Line: HCT116 (human colon cancer cell line)
Concentration: 400 μM
Incubation Time: 48 h
Result: Background: 94,863 m6A peaks containing transcripts of 13,577 genes in humantenine group, and found 4516 differential m6A-modified mRNAs and 3430 differentially expressed mRNAs, with 1401 genes overlapping between them.
KEGG and GO annotation terms for actin cytoskeleton, tight junctions, and adherens junctions were significantly enriched in these overlapping genes.
11 kinds of RNA m6A methylation regulators showed differential expression, including 4 writers, 6 readers and 1 eraser.
The m6A methylation levels of target genes related to tight junctions, adherens junctions and actin cytoskeleton regulation were disordered.
The m6A methylation level of IQGAP3 mRNA transcripts was decreased, and the mRNA stability and expression level of IQGAP3 were reduced.
Parmacokinetics
Species Dose Route AUC0-t AUC0-∞ MRT0-t MRT0-∞ T1/2 Vz Clearance (CL) Cmax
Rat[3] 0.1 mg/kg i.v. 14.7 ± 3.7 ng·h/mL 14.0 ± 3.7 ng·h/mL 1.2 ± 0.1 h 1.2 ± 0.1 h 1.5 ± 0.3 h 15.9 ± 4.9 L/kg 7.6 ± 2.3 L/h/kg 11.5 ± 3.6 ng/mL
In Vivo

Humantenine (0.1 mg/kg; i.v.; single dose) reaches a maximum plasma concentration of 11.5 ng/mL in male Sprague-Dawley rats, with an elimination half-life of 1.5 h[3].
Humantenine (0.1 g/kg, dose converted from total Gelsemium elegans powder; administered via oral gavage; single dose) reaches the peak time at 0.083 h in female SD rats, with an elimination half-life as long as 29.03 h, exhibiting pharmacokinetic characteristics of rapid absorption and slow elimination [4].

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

Animal Model: Sprague-Dawley (male, 200-220 g)[3]
Dosage: 0.1 mg/kg
Administration: i.v.; single dose
Result: Achieved AUC(0-t) = 14.7 ± 3.7 ng/mL*h.
Achieved AUC(0-∞) = 14.0 ± 3.7 ng/mL*h.
Achieved MRT(0-t) = 1.2 ± 0.1 h.
Achieved MRT(0-∞) = 1.2 ± 0.1 h.
Achieved t1/2z = 1.5 ± 0.3 h.
Achieved Vz = 15.9 ± 4.9 L/kg.
Achieved CLz/F = 7.6 ± 2.3 L/h/kg.
Achieved Cmax = 11.5 ± 3.6 ng/mL.
Molecular Weight

354.44

Formula

C21H26N2O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1N(C2=C(C=CC=C2)[C@@]13[C@@]4([H])C[C@]5([H])[C@@](CO4)([H])[C@](N(C/C5=C\C)C)([H])C3)OC
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Purity & Documentation
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

Humantenine Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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:

Humantenine82375-29-9Anaplastic lymphoma kinase (ALK)METTL3Anaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246Methyltransferase-like 3human liver microsomesliver microsomesdemethylationdehydrogenationmiceGelsemium elegansSprague-Dawley ratspig liver microsomesrat liver microsomesgoat liver microsomesInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Humantenine
Cat. No.:
HY-N4031
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

English - EN (251 KB) Français - FR (251 KB) Deutsch - DE (251 KB) Norwegian - NO (251 KB) Español - ES (251 KB) Swedish - SV (251 KB) Italian - IT (251 KB) Korean - KR (251 KB) Portuguese - PT (251 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.