1. Epigenetics
  2. Histone Methyltransferase
  3. CARM1-IN-1 hydrochloride

CARM1-IN-1 (compound 7g) hydrochloride is a highly potent and selective inhibitor of CARM1 (IC50=8.6 μM, CARM1/PABP1), with low inhibitory activity against PRMT1 and SET7 (IC50 >667 μM). CARM1-IN-1 hydrochloride inhibits the methylation activity of CARM1 and the methylation levels of different substrates, such as PABP1, CA150, SmB, and H3. CARM1-IN-1 hydrochloride also inhibits the promoter activity of prostate-specific antigen (PSA) without significant cytotoxicity.

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CARM1-IN-1 hydrochloride

CARM1-IN-1 hydrochloride 構造式

CAS 番号 : 2070018-31-2

容量 価格(税別) 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
5 mg $100 在庫あり
10 mg $160 在庫あり
25 mg $320 在庫あり
50 mg $520 在庫あり
100 mg $805 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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カスタマーレビュー

Based on 4 publication(s) in Google Scholar

Other Forms of CARM1-IN-1 hydrochloride:

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製品説明

CARM1-IN-1 (compound 7g) hydrochloride is a highly potent and selective inhibitor of CARM1 (IC50=8.6 μM, CARM1/PABP1), with low inhibitory activity against PRMT1 and SET7 (IC50 >667 μM). CARM1-IN-1 hydrochloride inhibits the methylation activity of CARM1 and the methylation levels of different substrates, such as PABP1, CA150, SmB, and H3. CARM1-IN-1 hydrochloride also inhibits the promoter activity of prostate-specific antigen (PSA) without significant cytotoxicity[1].

IC50 & Target

PRMT4

 

体外実験

CARM1-IN-1 (compound 7g) hydrochloride (100 μM; 90 min) inhibits CARM1-mediated methylation of different substrates (PABP1, CA150, SmB, and H3), such as Flag-PABP1 methylation, without inhibitory activity against HKMTs[1].
CARM1-IN-1 (compound 7g) hydrochloride (8 μM; 42-44 h) inhibits PSA promoter activity in luciferase assay in LNCaP cells, without affecting cell viability[1].

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

Cell Viability Assay[1]

Cell Line: PCR LNCa cells
Concentration: 1 μM, 2 μM, 4 μM, 6 μM, 8 μM
Incubation Time: 42-48 h
Result: Showed a significant dose-dependent reduction of the PSA promoter activity, at concentration that did not affect cell viability.
分子量

591.72

分子式

C26H22Br2ClNO3

CAS 番号
Appearance

Solid

Color

Light yellow to yellow

SMILES

[H]Cl.O=C1/C(CN(CC2=CC=CC=C2)C/C1=C\C3=CC=C(O)C(Br)=C3)=C/C4=CC=C(O)C(Br)=C4

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

4°C, sealed storage, away from moisture

*The compound is unstable in solutions, freshly prepared is recommended.

溶剤 & 溶解度
体外: 

DMSO : 250 mg/mL (422.50 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6900 mL 8.4499 mL 16.8999 mL
5 mM 0.3380 mL 1.6900 mL 3.3800 mL
10 mM 0.1690 mL 0.8450 mL 1.6900 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始)

C1

×
体積 (開始)

V1

=
濃度 (終了)

C2

×
体積 (終了)

V2

体内:

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 (4.22 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 (4.22 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 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 (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:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
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 compound is unstable in solutions, freshly prepared is recommended.

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.
純度とドキュメンテーション
参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.6900 mL 8.4499 mL 16.8999 mL 42.2497 mL
5 mM 0.3380 mL 1.6900 mL 3.3800 mL 8.4499 mL
10 mM 0.1690 mL 0.8450 mL 1.6900 mL 4.2250 mL
15 mM 0.1127 mL 0.5633 mL 1.1267 mL 2.8166 mL
20 mM 0.0845 mL 0.4225 mL 0.8450 mL 2.1125 mL
25 mM 0.0676 mL 0.3380 mL 0.6760 mL 1.6900 mL
30 mM 0.0563 mL 0.2817 mL 0.5633 mL 1.4083 mL
40 mM 0.0422 mL 0.2112 mL 0.4225 mL 1.0562 mL
50 mM 0.0338 mL 0.1690 mL 0.3380 mL 0.8450 mL
60 mM 0.0282 mL 0.1408 mL 0.2817 mL 0.7042 mL
80 mM 0.0211 mL 0.1056 mL 0.2112 mL 0.5281 mL
100 mM 0.0169 mL 0.0845 mL 0.1690 mL 0.4225 mL
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  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
× = ×
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.

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Inquiry Information

製品名:
CARM1-IN-1 hydrochloride
製品番号:
HY-12759A
数量:
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