2. Cell Cycle/DNA Damage
    Epigenetics
  3. HDAC
  4. TMP195

TMP195 

Cat. No.: HY-18361 Purity: 98.98%
COA Handling Instructions

TMP195 is a selective class IIa histone deacetylase (HDAC) inhibitor with Kis of 59, 60, 26, 15 nM for HDAC4, HDAC5, HDAC7 and HDAC9, respectively.

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

TMP195 Chemical Structure

TMP195 Chemical Structure

CAS No. : 1314891-22-9

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 145 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 145 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 132 In-stock
Estimated Time of Arrival: December 31
10 mg USD 228 In-stock
Estimated Time of Arrival: December 31
50 mg USD 792 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1320 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
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Customer Review

Based on 10 publication(s) in Google Scholar

Top Publications Citing Use of Products

View All HDAC Isoform Specific Products:

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

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

TMP195 is a selective class IIa histone deacetylase (HDAC) inhibitor with Kis of 59, 60, 26, 15 nM for HDAC4, HDAC5, HDAC7 and HDAC9, respectively.

IC50 & Target[1]

HDAC9

9 nM (IC50)

HDAC7

46 nM (IC50)

HDAC5

106 nM (IC50)

HDAC4

111 nM (IC50)

HDAC8

11700 nM (IC50)

HDAC6

47800 nM (IC50)

In Vitro

TMP195 blocks the accumulation of CCL2 protein in the supernatants of monocyte-derived macrophage differentiation cultures. TMP195 significantly increases the amount of CCL1 protein secreted by the monocytes compared to vehicle group. In the transcriptional profiling data from the PHA-stimulated PBMC experiments, CCL2 and CCL1 are respectively down- or upregulated by TMP195[1]. TMP195 occupies the acetyllysine-binding site of class IIa HDACs. TMP195 competes against binding of HDAC7 to a variety of side-chain modifications on the same peptide backbone, despite no interference with the activity of other acetyllysine reader proteins BRD4 (IC50>50 μM)[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo

TMP195 treatment alters the tumour microenvironment and reduces tumour burden and pulmonary metastases by modulating macrophage phenotypes. TMP195 induces the recruitment and differentiation of highly phagocytic and stimulatory macrophages within tumors. Combining TMP195 with chemotherapy regimens or T-cell checkpoint blockade in this model significantly enhances the durability of tumour reduction[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

456.42

Appearance

Solid

Formula

C23H19F3N4O3
CAS No.
SMILES

O=C(NCC(C)(C)C1=COC(C2=CC=CC=C2)=N1)C3=CC(C4=NOC(C(F)(F)F)=N4)=CC=C3
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 : ≥ 100 mg/mL (219.10 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1910 mL 10.9548 mL 21.9096 mL
5 mM 0.4382 mL 2.1910 mL 4.3819 mL
10 mM 0.2191 mL 1.0955 mL 2.1910 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 3 mg/mL (6.57 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 3 mg/mL (6.57 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 3 mg/mL (6.57 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.19%

COA (245 KB) LCMS (121 KB)

Handling Instructions (2659 KB)
References
Kinase Assay
[2]

Recombinant HDAC7 catalytic domain (amino acids 483-903) is labeled with DyLight 650 and applied to an arrayed library of 3,868 immobilized 20-mer peptides. Arrays are conducted using an automated TECAN HS4 microarray processing station, initiated by incubation with blocking buffer for 30 min at 30°C followed by ishing with saline containing 50 mM Tris Base and 0.1% Tween-20 (pH 7.2) before incubation with the labeled HDAC7 protein for 120 min at 4°C. In the case of TMP195 competition experiments, the labeled protein is pre-incubated with TMP195 for 30 min before application to the array. The microarrays are then ished before being dried and imaged with an scanner[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2]

Mice: For all mouse experiments, mice are treated with intraperitoneal (i.p.) injections of 50 μL of the vehicle dimethyl sulfoxide (DMSO) or 50 μL of TMP195 dissolved in 100% DMSO at a final concentration of 50 mg per kg daily[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References
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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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This equation is commonly abbreviated as: C1V1 = C2V2

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Keywords:

TMP1951314891-22-9TMP 195TMP-195HDACHistone deacetylasesInhibitorinhibitorinhibit

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