2. MAPK/ERK Pathway Stem Cell/Wnt TGF-beta/Smad
  3. ERK JNK TGF-beta/Smad
  4. (+)-Columbianetin

(+)-Columbianetin  (Synonyms: (S)-Columbianetin)

Cat. No.: HY-N0363 Purity: 99.04%
COA
SDS
Handling Instructions Technical Support

(+)-Columbianetin acts as an inhibitor of JNK and ERK as well as an activator of TGFβ signaling. (+)-Columbianetin inhibits UVA-induced phosphorylation of JNK and ERK, reduces the production of MMP-1, reverses UVA-induced collagen degradation, and alleviates UVA-mediated inhibition of Smad2/3 phosphorylation and translocation. (+)-Columbianetin regulates the AP-1 and ASK1-MAPK signaling pathways, inhibits the production of ROS, blocks sub-G1 cell cycle arrest, modulates the expression of MMP, and protects human keratinocytes against UVB-induced damage. (+)-Columbianetin is applicable to research related to skin aging.

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

(+)-Columbianetin

(+)-Columbianetin Chemical Structure

CAS No. : 3804-70-4

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 2 publication(s) in Google Scholar

Other Forms of (+)-Columbianetin:

(+)-Columbianetin Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

(+)-Columbianetin acts as an inhibitor of JNK and ERK as well as an activator of TGFβ signaling. (+)-Columbianetin inhibits UVA-induced phosphorylation of JNK and ERK, reduces the production of MMP-1, reverses UVA-induced collagen degradation, and alleviates UVA-mediated inhibition of Smad2/3 phosphorylation and translocation. (+)-Columbianetin regulates the AP-1 and ASK1-MAPK signaling pathways, inhibits the production of ROS, blocks sub-G1 cell cycle arrest, modulates the expression of MMP, and protects human keratinocytes against UVB-induced damage. (+)-Columbianetin is applicable to research related to skin aging[1][2].

In Vitro

(+)-Columbianetin (1-25 μM; 48 h) exhibits dose-dependent cytotoxicity in human dermal fibroblasts with an IC50 of 93.89 μM, and maintains >90% cell viability at concentrations up to 10 μM after 48 h incubation[1].
(+)-Columbianetin (1-10 μM) dose-dependently suppresses UVA (10 J/cm2)-induced reactive nitrogen species generation in human dermal fibroblasts[1].
(+)-Columbianetin (1-10 μM; 24 h) dose-dependently reverses UVA (10 J/cm2)-induced changes in human dermal fibroblasts, reducing MMP-1 release to 19,094 pg/mL and increasing type Iα1 pro-collagen release to 1,955 pg/mL at 10 μM after 24 h incubation[1].
(+)-Columbianetin (1-10 μM; 24 h) dose-dependently reverses UVA (10 J/cm2)-induced changes in human dermal fibroblasts, suppressing MMP-1 gene expression and increasing type I pro-collagen gene expression after 24 h incubation[1].
(+)-Columbianetin (1-10 μM; 48 h) dose-dependently reverses UVA (10 J/cm2)-induced changes in human dermal fibroblasts, suppressing MMP-1 protein expression and increasing type I pro-collagen and collagen protein expression after 48 h incubation[1].
(+)-Columbianetin (10 μM; 24 h) suppresses UVA (10 J/cm2)-induced phosphorylation of JNK and ERK, but not p38, in human dermal fibroblasts after 24 h incubation[1].
(+)-Columbianetin (10 μM; 24 h) reverses UVA (10 J/cm2)-induced changes in the TGFβ pathway in human dermal fibroblasts, increasing p-Smad2/3 and Smad4 protein levels and decreasing Smad7 protein levels after 24 h incubation[1].
(+)-Columbianetin (10 μM; 24 h) increases nuclear levels of p-Smad2/3 and Smad4, reversing UVA (10 J/cm2)-induced reductions in human dermal fibroblasts after 24 h incubation[1].
(+)-Columbianetin (1-20 μM; 24 h) dose-dependently increases the viability of UVB-exposed HaCaT cells, with near-full viability restoration at 20 μM after 24 h of treatment[2].
(+)-Columbianetin (1-20 μM; 24 h) dose-dependently reduces UVB-induced cell injury in HaCaT cells, with LDH release suppressed to ~20% of positive control levels at 20 μM after 24 h of treatment[2].
(+)-Columbianetin (1-20 μM; 2 h) dose-dependently scavenges H2O2-induced intracellular ROS in HaCaT cells, with ROS generation reduced to ~72% of H2O2-only levels at 20 μM after 2 h of treatment[2].
(+)-Columbianetin (1-20 μM; 24 h) dose-dependently scavenges UVB-induced intracellular ROS in HaCaT cells, with ROS generation reduced to ~72% of UVB-only levels at 20 μM after 24 h of treatment[2].
(+)-Columbianetin (1-20 μM; 24 h) dose-dependently reduces UVB-induced sub-G1 phase cell cycle arrest in HaCaT cells, with sub-G1 phase cell percentage lowered to 10.62% at 20 μM after 24 h of treatment[2].
(+)-Columbianetin (1-20 μM; 24 h) dose-dependently regulates UVB-altered gene expression of MMP-2, MMP-9, TIMP-1, and TIMP-2 in HaCaT cells after 24 h of treatment[2].
(+)-Columbianetin (1-20 μM; 24 h) dose-dependently regulates UVB-altered protein expression of MMP-2, MMP-9, TIMP-1, and TIMP-2 in HaCaT cells after 24 h of treatment[2].
(+)-Columbianetin (1-20 μM; 24 h) dose-dependently inhibits UVB-induced phosphorylation of p38, JNK, and ERK MAPKs in HaCaT cells, with the greatest inhibition observed at 20 μM after 24 h of treatment[2].
(+)-Columbianetin (1-20 μM; 24 h) dose-dependently inhibits UVB-induced phosphorylation of ASK1 in HaCaT cells, with p-ASK1 levels reduced to ~80% of UVB-only levels at 20 μM after 24 h of treatment[2].
(+)-Columbianetin (1-20 μM; 24 h) dose-dependently inhibits UVB-induced activation of the AP-1 component c-fos in HaCaT cells, with c-fos levels reduced to ~80% of UVB-only levels at 20 μM after 24 h of treatment[2].
(+)-Columbianetin (1-20 μM; 24 h) dose-dependently inhibits UVB-induced phosphorylation of p53 and upregulation of Bax in HaCaT cells, with the greatest inhibition observed at 20 μM after 24 h of treatment[2].

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

(+)-Columbianetin Related Antibodies

ELISA Assay[1]

Cell Line: UVA-irradiated human dermal fibroblasts (HDFs)
Concentration: 1-10 μM
Incubation Time: 24 h
Result: Reduced UVA-increased MMP-1 levels from 20,849 pg/mL to 19,094 pg/mL at 10 μM.
Increased UVA-decreased type Iα1 pro-collagen levels from 1,753 pg/mL to 1,955 pg/mL at 10 μM.

Real Time qPCR[1]

Cell Line: UVA-irradiated human dermal fibroblasts (HDFs)
Concentration: 1-10 μM
Incubation Time: 24 h
Result: Dose-dependently suppressed UVA-increased MMP-1 mRNA expression.
Dose-dependently increased UVA-decreased type I pro-collagen mRNA expression.

Western Blot Analysis[1]

Cell Line: UVA-irradiated human dermal fibroblasts (HDFs)
Concentration: 1-10 μM
Incubation Time: 48 h
Result: Dose-dependently suppressed UVA-increased MMP-1 protein expression.
Dose-dependently increased UVA-decreased type I pro-collagen and collagen protein expression.

Western Blot Analysis[1]

Cell Line: UVA-irradiated human dermal fibroblasts (HDFs)
Concentration: 10 μM
Incubation Time: 24 h
Result: Suppressed UVA-induced phosphorylation of JNK and ERK.
Did not significantly affect UVA-induced phosphorylation of p38.\nIncreased UVA-decreased p-Smad2/3 and Smad4 protein levels.
Decreased UVA-increased Smad7 protein levels.\nIncreased nuclear levels of p-Smad2/3 and Smad4, reversing UVA-induced reductions.

RT-PCR[2]

Cell Line: UVB-exposed human keratinocyte (HaCaT) cells
Concentration: 1-20 μM
Incubation Time: 24 h
Result: Reduced UVB-induced upregulation of MMP-2 and MMP-9 gene expression in a dose-dependent manner.
Inhibited UVB-induced downregulation of TIMP-1 and TIMP-2 gene expression in a dose-dependent manner.
Molecular Weight

246.26

Formula

C14H14O4
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C1C=CC2=CC=C(O[C@H](C(C)(O)C)C3)C3=C2O1
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

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

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (406.07 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 4.0607 mL 20.3037 mL 40.6075 mL
5 mM 0.8121 mL 4.0607 mL 8.1215 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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: ≥ 2.5 mg/mL (10.15 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (10.15 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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).

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

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: 99.04%

SDS (393 KB)

COA (252 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
References

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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.0607 mL 20.3037 mL 40.6075 mL 101.5187 mL
5 mM 0.8121 mL 4.0607 mL 8.1215 mL 20.3037 mL
10 mM 0.4061 mL 2.0304 mL 4.0607 mL 10.1519 mL
15 mM 0.2707 mL 1.3536 mL 2.7072 mL 6.7679 mL
20 mM 0.2030 mL 1.0152 mL 2.0304 mL 5.0759 mL
25 mM 0.1624 mL 0.8121 mL 1.6243 mL 4.0607 mL
30 mM 0.1354 mL 0.6768 mL 1.3536 mL 3.3840 mL
40 mM 0.1015 mL 0.5076 mL 1.0152 mL 2.5380 mL
50 mM 0.0812 mL 0.4061 mL 0.8121 mL 2.0304 mL
60 mM 0.0677 mL 0.3384 mL 0.6768 mL 1.6920 mL
80 mM 0.0508 mL 0.2538 mL 0.5076 mL 1.2690 mL
100 mM 0.0406 mL 0.2030 mL 0.4061 mL 1.0152 mL
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(+)-Columbianetin Related Classifications

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  • 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:

(+)-Columbianetin3804-70-4(S)-ColumbianetinERKJNKTGF-beta/SmadExtracellular signal regulated kinasesc-Jun N-terminal kinaseTransforming growth factor betaMMP-1Smad2/3HaCaT cellsAP-1UVAhuman keratinocytesTGFβ signalingASK1-MAPK signaling pathwaysInhibitorinhibitorinhibit

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