1. Vitamin D Related/Nuclear Receptor Autophagy
  2. p62 Nuclear Hormone Receptor 4A/NR4A
  3. Triptohypol C

Triptohypol C, a Tripterin (HY-13067) derivative, is a potent Nur77-targeting anti-inflammatory agent with an Kd value of 0.87 μM. Triptohypol C inhibits inflammatory response by promoting the interactions of Nur77 with TRAF2 and p62/SQSTM1.

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Triptohypol C Chemical Structure

Triptohypol C Chemical Structure

CAS No. : 193957-88-9

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Description

Triptohypol C, a Tripterin (HY-13067) derivative, is a potent Nur77-targeting anti-inflammatory agent with an Kd value of 0.87 μM. Triptohypol C inhibits inflammatory response by promoting the interactions of Nur77 with TRAF2 and p62/SQSTM1[1].

IC50 & Target

Nur77/NR4A1

 

Cellular Effect
Cell Line Type Value Description References
A549 IC50
3.15 μM
Compound: 2
Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
[PMID: 28865279]
A549 IC50
3.15 μM
Compound: 2
Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
[PMID: 28688281]
MIA PaCa-2 IC50
0.72 μM
Compound: 2
Antiproliferative activity against human MIAPaCa2 cells after 72 hrs by MTT assay
Antiproliferative activity against human MIAPaCa2 cells after 72 hrs by MTT assay
[PMID: 28865279]
MIA PaCa-2 IC50
0.72 μM
Compound: 2
Antiproliferative activity against human MIAPaCa2 cells after 72 hrs by MTT assay
Antiproliferative activity against human MIAPaCa2 cells after 72 hrs by MTT assay
[PMID: 28688281]
In Vitro

Triptohypol C (compound 3a) (2 μM; 1 h) strongly antagonize the effect of TNFα on inducing IκBα degradation, and inhibits inflammatory response by promoting the interactions of Nur77 with TRAF2 and p62/SQSTM1[1].
Triptohypol C (2 μM; 10 h) cause 3.12% apoptosis in HepG2 cells, which is less toxic than Tripterin[1].

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

Western Blot Analysis[1]

Cell Line: Lysates from HepG2 cells (incubated with 20 ng/mL TNFα for 30 min)
Concentration: 2 μM
Incubation Time: 1 h
Result: Strongly antagonized the effect of TNFα on inducing IκBα degradation

Immunofluorescence[1]

Cell Line: HepG2 cells (transfected with Myc-Nur77 and Flag-TRAF2 or Flag-p62)
Concentration: 2 μM
Incubation Time: 1 h
Result: Promoted the interactions between Nur77 and TRAF2 and p62/SQSTM1.

Apoptosis Analysis[1]

Cell Line: HepG2 cells
Concentration: 2 μM
Incubation Time: 10 h
Result: Caused 3.12% apoptosis in cells, which was less cytotoxic than Tripterin (>10%).
In Vivo

Caused 3.12% apoptosis in cells, which was less cytotoxic than Tripterin (>10%).

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

Animal Model: Zebrafish[1]
Dosage: 0.5 μM, 1 μM and 1.25 μM
Administration: 72 h
Result: Had less effect than Tripterin on the death rate and malformation of zebrafish either at a concentration of 1.25 μM for 24 h or at a concentration of 0.5 μM for 72 h.
Molecular Weight

452.63

Formula

C29H40O4

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

CC1=C(O)C(O)=CC2=C1CC=C3[C@@]2(C)CC[C@]4(C)[C@]3(C)CC[C@]5(C)[C@@]4([H])C[C@](C)(C(O)=O)CC5

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)

Solvent & Solubility
In Vitro: 

DMSO : 16.67 mg/mL (36.83 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 2.2093 mL 11.0465 mL 22.0931 mL
5 mM 0.4419 mL 2.2093 mL 4.4186 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.

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In Vivo Dissolution Calculator
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Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 95.44%

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 2.2093 mL 11.0466 mL 22.0931 mL 55.2328 mL
5 mM 0.4419 mL 2.2093 mL 4.4186 mL 11.0466 mL
10 mM 0.2209 mL 1.1047 mL 2.2093 mL 5.5233 mL
15 mM 0.1473 mL 0.7364 mL 1.4729 mL 3.6822 mL
20 mM 0.1105 mL 0.5523 mL 1.1047 mL 2.7616 mL
25 mM 0.0884 mL 0.4419 mL 0.8837 mL 2.2093 mL
30 mM 0.0736 mL 0.3682 mL 0.7364 mL 1.8411 mL
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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.

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Product Name:
Triptohypol C
Cat. No.:
HY-117469
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