2. Cell Cycle/DNA Damage PROTAC Epigenetics Apoptosis Neuronal Signaling Autophagy Immunology/Inflammation NF-κB Metabolic Enzyme/Protease
  3. HDAC PROTACs Apoptosis PINK1/Parkin Autophagy Reactive Oxygen Species (ROS)
  4. JPS016 TFA

JPS016 TFA is a class I histone deacetylase (HDAC) PROTAC inhibitor. JPS016 TFA recruits the VHL E3 ligase (Ligands for E3 Ligase) to mediate the ubiquitination and proteasomal degradation of HDAC1, HDAC2 and HDAC3. JPS016 TFA reduces the viability of colon cancer cells and induces Apoptosis. JPS016 TFA activates the PINK1/Parkin mitochondrial Autophagy pathway, enhances cardiomyocyte viability, alleviates mitochondrial damage, and reduces mitochondrial ROS production in cells. JPS016 TFA is applicable to research related to colon cancer and sepsis cardiomyopathy.
(Pink: HDAC ligand (HY-50934); Blue: VHL ligand (HY-125845); Black: linker (HY-175977)).

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

JPS016 TFA

JPS016 TFA Chemical Structure

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

Other Forms of JPS016 TFA:

JPS016 TFA Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE JPS016 TFA

View All HDAC Isoform Specific Products:

View All Isoforms
HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

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View All Isoforms
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

JPS016 TFA is a class I histone deacetylase (HDAC) PROTAC inhibitor. JPS016 TFA recruits the VHL E3 ligase (Ligands for E3 Ligase) to mediate the ubiquitination and proteasomal degradation of HDAC1, HDAC2 and HDAC3. JPS016 TFA reduces the viability of colon cancer cells and induces Apoptosis. JPS016 TFA activates the PINK1/Parkin mitochondrial Autophagy pathway, enhances cardiomyocyte viability, alleviates mitochondrial damage, and reduces mitochondrial ROS production in cells. JPS016 TFA is applicable to research related to colon cancer and sepsis cardiomyopathy[1][2]. (Pink: HDAC ligand (HY-50934); Blue: VHL ligand (HY-125845); Black: linker (HY-175977)).

In Vitro

JPS016 (Compound 9) (0.001-100 μM; 24 h) TFA potently degrades HDAC1 (DC50 = 0.55 μM, Dmax = 77%) and HDAC3 (DC50 = 0.53 ± 0.13 μM, Dmax = 66%) in HCT116 cells after 24 h of treatment[1].
JPS016 (10 μM; 2-48 h) TFA upregulates the acetylation level of histone H3K56 in HCT116 cells in a time-dependent manner in vitro, with the acetylation peak occurring at 36 h[1].
JPS016 (1-10 μM; 24-48 h) TFA reduces the stability of LSD1 and SIN3A, components of the HDAC1/2 corepressor complex, in HCT116 cells[1].
JPS016 (0.1-100 μM; 48 h) TFA reduces the viability of HCT116 cells, with an EC50 of 5.3 μM after 48 h of treatment[1].
JPS016 (10 μM; 24-48 h) TFA induces apoptosis in HCT116 cells. After 48 h of treatment, 70% of cells are present in the apoptotic sub-G1 population, and the drug significantly enriches genes related to cell cycle arrest and apoptosis[1].
JPS016 (24 h) TFA protects HL-1 mouse cardiomyocytes against LPS (HY-D1056)-induced injury by restoring cell viability and reducing cytotoxicity, and decreases LPS-induced mitochondrial ROS production in cells[2].
JPS016 (0.01-10 μM) TFA induces dose-dependent degradation of class I HDACs in both untreated and LPS-stimulated HL-1 mouse cardiomyocytes, with preferential activity against HDAC1, HDAC3 and HDAC8[2].
JPS016 (24 h) TFA enhances histone acetylation and lactylation modifications in HL-1 mouse cardiomyocytes. Specifically, under LPS-induced SCM stress conditions, it reverses the LPS-induced pathogenic gene program, regulates mitochondria-related cellular processes in HL-1 mouse cardiomyocytes, and promotes exosome formation and mitochondrial extrusion in HL-1 mouse cardiomyocytes under LPS-induced SCM stress[2].
JPS016 (administered for 24 h) TFA activates the PINK1/Parkin mitophagy pathway in HL-1 mouse cardiomyocytes under LPS-induced SCM stress[2].

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

JPS016 TFA Related Antibodies

Western Blot Analysis[1]

Cell Line: HCT116 human colon carcinoma cells
Concentration: 0.01-10 μM (24 h dose-response); 10 μM (time-course)
Incubation Time: 2-48 h (time-course); 24 h (dose-response)
Result: Reduced HDAC1 to 25%, HDAC2 to 50%, HDAC3 to 50% at 0.1 μM for 24 h.
Reduced HDAC1 to 25%, HDAC2 to 75%, HDAC3 to 25% at 1 μM for 24 h.
Reduced HDAC1 to 25%, HDAC2 to 75%, HDAC3 to ~100% (hook effect) at 10 μM for 24 h.
Reached 84% degradation of HDAC1 and 51% degradation of HDAC2 by 48 h at 10 μM.
Reached ~50% degradation of HDAC3 at 36 and 48 h at 10 μM.
Showed DC50 values of 0.55 ± 0.18 μM (HDAC1) and 0.53 ± 0.13 μM (HDAC3), with Dmax values of 77% (HDAC1), 45% (HDAC2), 66% (HDAC3) after 24 h dose-response testing.

Apoptosis Analysis[1]

Cell Line: HCT116 human colon carcinoma cells
Concentration: 10 μM
Incubation Time: 24, 48 h
Result: Induced 30% of cells in apoptotic sub-G1 population at 24 h.
Induced 70% of cells in apoptotic sub-G1 population at 48 h.
Molecular Weight

1012.14

Formula

C50H64F3N7O10S
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(N(C[C@@H]1O)[C@@H](C1)C(NCC2=CC=C(C(SC=N3)=C3C)C=C2)=O)[C@H](C(C)(C)C)NC(COCCCCCCCCCOCC(NC(C=C4)=CC=C4C(NC(C=CC=C5)=C5N)=O)=O)=O.OC(C(F)(F)F)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, protect from light, stored under nitrogen

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

Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (98.80 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.9880 mL 4.9400 mL 9.8801 mL
5 mM 0.1976 mL 0.9880 mL 1.9760 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, stored under nitrogen). 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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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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This equation is commonly abbreviated as: C1V1 = C2V2

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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.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
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, stored under nitrogen). 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 0.9880 mL 4.9400 mL 9.8801 mL 24.7001 mL
5 mM 0.1976 mL 0.9880 mL 1.9760 mL 4.9400 mL
10 mM 0.0988 mL 0.4940 mL 0.9880 mL 2.4700 mL
15 mM 0.0659 mL 0.3293 mL 0.6587 mL 1.6467 mL
20 mM 0.0494 mL 0.2470 mL 0.4940 mL 1.2350 mL
25 mM 0.0395 mL 0.1976 mL 0.3952 mL 0.9880 mL
30 mM 0.0329 mL 0.1647 mL 0.3293 mL 0.8233 mL
40 mM 0.0247 mL 0.1235 mL 0.2470 mL 0.6175 mL
50 mM 0.0198 mL 0.0988 mL 0.1976 mL 0.4940 mL
60 mM 0.0165 mL 0.0823 mL 0.1647 mL 0.4117 mL
80 mM 0.0124 mL 0.0618 mL 0.1235 mL 0.3088 mL
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JPS016 TFA Related Classifications

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:

JPS016JPS 016JPS-016HDACPROTACsApoptosisPINK1/ParkinAutophagyReactive Oxygen Species (ROS)Histone deacetylasesPTEN-induced kinase 1/ParkinPROTACapoptosisInhibitorinhibitorinhibit

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