2. Vitamin D Related/Nuclear Receptor Apoptosis Epigenetics
  3. Progesterone Receptor Apoptosis Glycosyltransferase
  4. AG-205

AG-205 is a progesterone receptor membrane component 1 (PGRMC1) antagonist and CGT inhibitor, with an IC50 of 50 μM against rat CGT. AG-205 exhibits antimitotic, antimigratory and anti-invasive activities. AG-205 increases the expression of genes encoding cholesterol biosynthesis pathway or steroidogenic enzymes. AG-205 promotes the regulation of cell cycle by apoptosis and reduces the migratory and invasive capacities of ovarian and breast cancer cells. AG-205 can be used in research related to renal cancer and breast cancer.

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AG-205

AG-205 Chemical Structure

CAS No. : 1375078-57-1

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AG-205 Related Antibodies

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Description

AG-205 is a progesterone receptor membrane component 1 (PGRMC1) antagonist and CGT inhibitor, with an IC50 of 50 μM against rat CGT. AG-205 exhibits antimitotic, antimigratory and anti-invasive activities. AG-205 increases the expression of genes encoding cholesterol biosynthesis pathway or steroidogenic enzymes. AG-205 promotes the regulation of cell cycle by apoptosis and reduces the migratory and invasive capacities of ovarian and breast cancer cells. AG-205 can be used in research related to renal cancer and breast cancer[1][2][3].

In Vitro

AG-205 (10-40 μM; 24 h) significantly increases the survival rate of SMKT-R3 human renal cancer cells[1].
AG-205 (2-10 μM) specifically reduces sulfatide levels in SMKT-R3 human renal cancer cells, with no effect on major non-sphingolipids[1].
AG-205 (10 μM; 6 h) specifically inhibits the synthesis of CGT-dependent galactolipids (GalC, MGDG) and sulfatides in CHO-CGT and CHO-Sulf cells expressing galactosylceramide synthase, while promoting the synthesis of GlcC[1].
AG-205 (10 μM; 48 h) inhibits the synthesis of GalC and MGDG and promotes the synthesis of GlcC in CHO-CGT cells, and this effect is independent of the expression of PGRMC1 or PGRMC2[1].
AG-205 (50 μM; 30 min) significantly inhibits the in vitro activity of UDP-galactose:ceramide galactosyltransferase (CGT) derived from CHO-CGT cells[1].
Pretreatment with AG-205 (50 μM; 24 h) abolishes the anti-apoptotic effect of progesterone against H2O2-induced cell death in human granulosa/luteal cells[2].
AG-205 (50 μM; overnight) reduces the nuclear localization level of PGRMC1 in human granulosa/luteal cells, with most PGRMC1 retained in the cytoplasm[2].
AG-205 (50 μM; overnight) increases the cytoplasmic level of HRK protein in human granulosa/luteal cells[2].
AG-205 (50 μM; overnight) disrupts the colocalization of cytochrome c with mitochondria in human granulosa/luteal cells, but does not alter the total level of cytochrome c in the cells[2].
AG-205 (50 μM; overnight) enhances the interaction between PGRMC1 and PGRMC2 in human granulosa/luteal cells, as evidenced by a 2.3-fold increase in PLA dots per cell[2].
AG-205 (50 μM; overnight) increases the expression level of Hrk mRNA by 6-8 folds in human granulosa/luteal cells, while slightly elevating the mRNA expression levels of several anti-apoptotic genes by 1.5-3 folds[2].
AG-205 (15 μM; 32 h) significantly upregulates the mRNA expression levels of genes encoding cholesterol biosynthetic enzymes, the sterol regulatory factor INSIG1, and steroidogenic enzymes in human endometrial T-HESC and HEC-1A cell lines[3].
AG-205 (15 μM; 80 h) upregulates the mRNA expression of HSD17B7, MSMO1 and INSIG1 in human endometrial T-HESC and HEC-1A cell lines, and this process is independent of PGRMC1 expression[3].
AG-205 (15 μM; 80 h) upregulates the mRNA expression of HSD17B7, MSMO1, and INSIG1 in human endometrial T-HESC and HEC-1A cell lines, and this process is independent of the expression of all four members of the MAPR family (PGRMC1, PGRMC2, NENF, CYB5D2)[3].
AG-205 (15 μM; 32 h) does not alter the mRNA or protein expression levels of PGRMC1 in the human endometrial T-HESC and HEC-1A cell lines, nor does it change the subcellular localization of PGRMC1 in these cell lines[3].

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

AG-205 Related Antibodies

Apoptosis Analysis[2]

Cell Line: human granulosa/luteal cells
Concentration: 50 μM
Incubation Time: 24 h (pretreatment)
Result: Eliminated progesterone's ability to attenuate H2O2-induced apoptosis, resulting in a dead cell/total cell ratio equivalent to H2O2 treatment alone.

Immunofluorescence[2]

Cell Line: human granulosa/luteal cells
Concentration: 50 μM
Incubation Time: overnight
Result: Reduced nuclear localization of PGRMC1; 31 ± 10% of cells showed nuclear PGRMC1 staining, compared to 67 ± 8% in controls.
Prominently localized PGRMC1 to the cytoplasm in treated cells.\nIncreased levels of HRK protein in the cytoplasm of treated cells, visible as enhanced green fluorescence compared to controls.\nAltered the subcellular localization of cytochrome c, with a portion of cytochrome c no longer co-localizing with mitochondria (visible as diffuse green fluorescence in the cytoplasm) instead of being restricted to punctate mitochondrial foci.
Left total cellular cytochrome c levels unchanged relative to controls.

Western Blot Analysis[2]

Cell Line: human granulosa/luteal cells
Concentration: 50 μM
Incubation Time: overnight
Result: Increased abundance of the ~27 kDa monomeric form of PGRMC1.
Decreased abundance of the higher molecular weight forms ≥50 kDa (dimers/oligomers) of PGRMC1.

Real Time qPCR[2]

Cell Line: human granulosa/luteal cells
Concentration: 50 μM
Incubation Time: overnight
Result: Induced a 6 to 8 fold increase in Harakiri (Hrk) mRNA levels.
Induced 1.5 to 3 fold increases in mRNA levels of Bag1, Bcl2A1, Birc3, Mcl1, and XIAP.
Induced a small increase in Casp4 mRNA.

Cell Viability Assay[3]

Cell Line: human endometrial T-HESC, HEC-1A
Concentration: 5 μM, 15 μM, 30 μM, 45 μM
Incubation Time: 24 h, 32 h, 48 h
Result: Had no effect on cell viability in either cell line for up to 48 h when used at 5 μM or 15 μM.

Real Time qPCR[3]

Cell Line: human endometrial T-HESC, HEC-1A
Concentration: 15 μM
Incubation Time: 32 h
Result: Significantly upregulated mRNA expression of multiple enzymes involved in cholesterol biosynthesis, including ACAT2, AACS, HMGCS1, HMGCR, MVK, PMVK, MVD, IDI1, FDPS, FDFT1, SQLE, LSS, CYP51A1, TM7SF2, MSMO1, NSDHL, HSD17B7, EBP, SC5D, DHCR7, and DHCR24, in both cell lines.
Upregulated mRNA expression of INSIG1 (a sterol-sensitive regulator) and steroidogenesis-related enzymes AKR1C1 and HSD17B14 in both cell lines.
Confirmed significant upregulation of HSD17B7, MSMO1, and INSIG1 in both cell lines via qPCR.

Real Time qPCR[3]

Cell Line: human endometrial T-HESC, HEC-1A (with prior siRNA-mediated knockdown of PGRMC1)
Concentration: 15 μM
Incubation Time: 32 h (following 48 h siRNA transfection)
Result: Induced a ~3 to 4-fold mean increase in HSD17B7, MSMO1, and INSIG1 mRNA expression in HEC-1A cells, and a ~4 to 6-fold mean increase in T-HESC cells.
Maintained identical upregulation in cells transfected with PGRMC1-targeting siRNA or control siRNA.

Real Time qPCR[3]

Cell Line: human endometrial T-HESC, HEC-1A (with prior siRNA-mediated knockdown of all four MAPR family members: PGRMC1, PGRMC2, NENF, CYB5D2)
Concentration: 15 μM
Incubation Time: 32 h (following 48 h siRNA transfection)
Result: Significantly upregulated mRNA expression of HSD17B7, MSMO1, and INSIG1 in both cell lines.
Maintained upregulation at the same magnitude in cells transfected with the MAPR-targeting siRNA mixture as in control siRNA-transfected cells.
Molecular Weight

454.98

Formula

C22H23ClN6OS
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC1=CC2=C(C=C1)N([C@@]3([H])[C@]2([H])CN(CC3)C)C(CSC4=NN=NN4C5=CC=C(C=C5)Cl)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 10 mg/mL (21.98 mM; ultrasonic and warming and heat to 60°C; 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 2.1979 mL 10.9895 mL 21.9790 mL
5 mM 0.4396 mL 2.1979 mL 4.3958 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. 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:

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: 1 mg/mL (2.20 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 1 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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% Corn Oil

    Solubility: 1 mg/mL (2.20 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 1 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
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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).
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%

SDS (251 KB)

COA (257 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. 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 2.1979 mL 10.9895 mL 21.9790 mL 54.9475 mL
5 mM 0.4396 mL 2.1979 mL 4.3958 mL 10.9895 mL
10 mM 0.2198 mL 1.0989 mL 2.1979 mL 5.4947 mL
15 mM 0.1465 mL 0.7326 mL 1.4653 mL 3.6632 mL
20 mM 0.1099 mL 0.5495 mL 1.0989 mL 2.7474 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.

Keywords:

AG-2051375078-57-1AG205AG 205Progesterone ReceptorApoptosisGlycosyltransferaseNR3C3galactosylceramidebreast cellsratrenal cancerCGTPGRMC1monogalactosyldiacylglycerolPGRMC2ovarian cellssulfatideInhibitorinhibitorinhibit

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