2. Epigenetics PI3K/Akt/mTOR
  3. Histone Methyltransferase Akt
  4. SETDB1-TTD-IN-1

SETDB1-TTD-IN-1 is a SETDB1 methyltransferase activator and SETDB1-TTD competitive inhibitor (Kd of 88 nM), and selectivity for SETDB1-TTD over other tudor and bromodomain proteins. SETDB1-TTD-IN-1 stimulates methyltransferase activity via increased catalytic activity, promotes Akt1 Lys64 methylation, Akt1 Thr308 phosphorylation and activation. SETDB1-TTD-IN-1 prevents SETDB1-TTD-histone H3 peptide association, induces global gene expression changes, exhibits cellular target engagement, and acts as a tool compound for SETDB1-TTD function exploration. SETDB1-TTD-IN-1 can be used for the research of breast cancer.

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SETDB1-TTD-IN-1

SETDB1-TTD-IN-1 Chemical Structure

CAS No. : 2755823-12-0

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of SETDB1-TTD-IN-1:

SETDB1-TTD-IN-1 Related Antibodies

Top Publications Citing Use of Products

View All Histone Methyltransferase Isoform Specific Products:

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EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 NSD3/WHSC1L1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

View All Akt Isoform Specific Products:

View All Isoforms
Akt Akt1 Akt2 Akt3

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

SETDB1-TTD-IN-1 is a SETDB1 methyltransferase activator and SETDB1-TTD competitive inhibitor (Kd of 88 nM), and selectivity for SETDB1-TTD over other tudor and bromodomain proteins. SETDB1-TTD-IN-1 stimulates methyltransferase activity via increased catalytic activity, promotes Akt1 Lys64 methylation, Akt1 Thr308 phosphorylation and activation. SETDB1-TTD-IN-1 prevents SETDB1-TTD-histone H3 peptide association, induces global gene expression changes, exhibits cellular target engagement, and acts as a tool compound for SETDB1-TTD function exploration. SETDB1-TTD-IN-1 can be used for the research of breast cancer[1][2].

IC50 & Target[2][1]

SETDB1/KMT2G

 

Akt1

 

In Vitro

SETDB1-TTD-IN-1 (R,R)-59) binds to the purified SETDB1 triple tudor domain with an IC50 of 1.7 μM in a competition TR-FRET assay[1].
SETDB1-TTD-IN-1 binds directly to the purified SETDB1 triple tudor domain with a Kd of 4.8 μM in an SPR assay[1].
SETDB1-TTD-IN-1 (0-100 μM; 60 min) increases full-length SETDB1-mediated methylation of the Akt1-K64 peptide in vitro with an EC50 of 19 μM, enhancing catalytic efficiency by increasing k_cat without altering SAM binding affinity[1].
SETDB1-TTD-IN-1 (2-40 μM; 1-24 h) promotes dose-dependent and time-dependent Akt1 trimethylation and T308 phosphorylation in HA-tagged Akt1-transfected HEK293T cells[1].
SETDB1-TTD-IN-1 (2-40 μM) promotes Akt1 trimethylation and T308 phosphorylation in HA-tagged Akt1-stably expressing DLD1 colorectal adenocarcinoma cells[1].
SETDB1-TTD-IN-1 (2.5-5 μM; 72 h) promotes proliferation of MDA-MB-231 breast cancer cells at concentrations of 2.5 μM and 5 μM after 72 hours of treatment[1].
SETDB1-TTD-IN-1 potently binds purified SETDB1-TTD with a Kd of 0.088 μM as measured by ITC assay[2].
SETDB1-TTD-IN-1 binds purified SETDB1-TTD with a Kd of 0.106 μM as measured by SPR[2].
SETDB1-TTD-IN-1 (100 μM) is highly selective for SETDB1-TTD, showing minimal to no activity against 14 other tudor domains, weak activity against 53BP1-TTD and JMJD2A-TTD, and no or very weak activity against 32 BRD proteins[2].
SETDB1-TTD-IN-1 completely blocks the binding of modified histone H3 peptides (H3K9me/K14ac, H3K9me2/K14ac, H3K9me3/K14ac) to purified SETDB1-TTD after 20 minutes of pretreatment[2].
SETDB1-TTD-IN-1 (0.01-100 μM) potently inhibits the interaction of purified SETDB1-TTD with biotinylated H3K9me2/K14ac (IC50 = 0.93 μM) and H3K9me3/K14ac (IC50 = 0.75 μM) peptides in an HTRF assay[2].
SETDB1-TTD-IN-1 (2.5-40 μM; 6 h) dose-dependently stabilizes SETDB1-TTD protein in SETDB1-TTD-transfected HEK293T cells at concentrations ≥5 μM after 6 hours of treatment[2].
SETDB1-TTD-IN-1 (6 μM; 18 h) increases the mobility of EGFP-tagged wild-type SETDB1-TTD in HEK293T cells after 18 hours of treatment, as shown by a significantly reduced FRAP normalized half-life recovery time[2].
SETDB1-TTD-IN-1 (10 μM; 24 h) significantly alters the expression of 72 genes, including 49 uniquely regulated genes, in THP-1 human acute monocytic leukemia cells after 24 hours of treatment[2].

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

SETDB1-TTD-IN-1 Related Antibodies

Western Blot Analysis[1]

Cell Line: HEK293T cells (transiently expressing HA-tagged Akt1)
Concentration: 2 μM, 5 μM, 10 μM, 20 μM, 40 μM
Incubation Time: 1 h; 2 h; 4 h; 24 h
Result: Triggered a dose-dependent and time-dependent increase in Akt1 trimethylation and T308 phosphorylation.

Cell Proliferation Assay[1]

Cell Line: MDA-MB-231 breast cancer cells
Concentration: 2.5-5 μM
Incubation Time: 72 h
Result: Stimulated cell proliferation at 2.5 μM and 5 μM; this effect was not observed at doses greater than 5 μM.
Molecular Weight

469.58

Formula

C28H31N5O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CN1C[C@@H](C2=CC=C(OCC3=CC=CC=C3)C=C2)C[C@@H](NC4=NC5=C(C(N4CC=C)=O)NC=C5)C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°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 : 125 mg/mL (266.20 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 2.1296 mL 10.6478 mL 21.2956 mL
5 mM 0.4259 mL 2.1296 mL 4.2591 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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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    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (4.43 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

  • Protocol 2

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 1.98 mg/mL (4.22 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.98 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (19.8 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.
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).

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

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: 99.93%

SDS (393 KB)

COA (248 KB) HNMR (240 KB) LCMS (95 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, 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 2.1296 mL 10.6478 mL 21.2956 mL 53.2391 mL
5 mM 0.4259 mL 2.1296 mL 4.2591 mL 10.6478 mL
10 mM 0.2130 mL 1.0648 mL 2.1296 mL 5.3239 mL
15 mM 0.1420 mL 0.7099 mL 1.4197 mL 3.5493 mL
20 mM 0.1065 mL 0.5324 mL 1.0648 mL 2.6620 mL
25 mM 0.0852 mL 0.4259 mL 0.8518 mL 2.1296 mL
30 mM 0.0710 mL 0.3549 mL 0.7099 mL 1.7746 mL
40 mM 0.0532 mL 0.2662 mL 0.5324 mL 1.3310 mL
50 mM 0.0426 mL 0.2130 mL 0.4259 mL 1.0648 mL
60 mM 0.0355 mL 0.1775 mL 0.3549 mL 0.8873 mL
80 mM 0.0266 mL 0.1331 mL 0.2662 mL 0.6655 mL
100 mM 0.0213 mL 0.1065 mL 0.2130 mL 0.5324 mL
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SETDB1-TTD-IN-1 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:

SETDB1-TTD-IN-12755823-12-0Histone MethyltransferaseAktPKBProtein kinase BDLD1 colorectal adenocarcinoma cellsbromodomain proteinsAkt1SETDB1 methyltransferaseTHP-1 human acute monocytic leukemia cellsSETDB1-TTDMDA-MB-231 breast cancer cellshuman SETDB1histone H3 peptideHEK293T cellsInhibitorinhibitorinhibit

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