TMP195 |
رقم الكتالوجGC19360
One-Click Copy Product Info
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TMP195 هو مثبط انتقائي من الدرجة IIa هيستون ديستيلاز (HDAC) مع Kis 59 ، 60 ، 26 ، 15 نانومتر لـ HDAC4 ، HDAC5 ، HDAC7 و HDAC9 ، على التوالي
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1314891-22-9
Sample solution is provided at 25 µL, 10mM.
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TMP195 is a selective class IIa histone deacetylase (HDAC) inhibitor with IC50 values of 0.111, 0.106, 47.8, 0.046, 11.7, and 0.009µM for HDAC4, 5, 6, 7, 8, and 9, respectively[1]. TMP195 binds to the drug-binding pockets of drug transporters ABCB1 and ABCG2, stimulating ATPase activity and weakening the drug efflux function of ABCB1 and ABCG2, thereby reversing the multidrug resistance mediated by ABCB1 and ABCG2[2]. TMP195 has been widely used to inhibit the growth of transplanted tumors and to develop combined therapies for effectively killing tumors[3].
In vitro, TMP195 treatment (25µM) for 48 hours significantly induced apoptosis and cell cycle arrest in H460 and H1703 cells, and led to mitochondrial dysfunction[4].
In vivo, TMP195 treatment significantly suppressed the growth of tumors in the MC38 xenograft mouse model by intraperitoneal injection at a dosage of 50mg/kg/day for 15 days and promoted the secretion of M1-type macrophage-related cytokines[5]. A single intraperitoneal injection of 50mg/kg TMP195 for 24 hours improved renal dysfunction in a mouse model of acute kidney injury (AKI) induced by lipopolysaccharide (LPS), reduced macrophage infiltration, and decreased the expression of cytokines and chemokines[6]. Daily intraperitoneal injection of TMP195 (50mg/kg) reduced the tumor burden and decreased lung metastasis in MMTV-PyMT tumor-bearing mice over a period of 13 days[7].
References:
[1] Lobera M, Madauss K P, Pohlhaus D T, et al. Selective class IIa histone deacetylase inhibition via a nonchelating zinc-binding group[J]. Nature chemical biology, 2013, 9(5): 319-325.
[2] Wu C P, Lusvarghi S, Wang J C, et al. The selective class IIa histone deacetylase inhibitor TMP195 resensitizes ABCB1-and ABCG2-overexpressing multidrug-resistant cancer cells to cytotoxic anticancer drugs[J]. International journal of molecular sciences, 2019, 21(1): 238.
[3] Cassetta L, Pollard J W. Repolarizing macrophages improves breast cancer therapy[J]. Cell research, 2017, 27(8): 963-964.
[4] Park J, Chen Y Y, Cao J J, et al. MYC plus class IIa HDAC inhibition drives mitochondrial dysfunction in non-small cell lung cancer[J]. Cell Reports, 2025, 44(6).
[5] Han Y, Sun J, Yang Y, et al. TMP195 exerts antitumor effects on colorectal cancer by promoting M1 macrophages polarization[J]. International journal of biological sciences, 2022, 18(15): 5653.
[6] Zhang W, Guan Y, Bayliss G, et al. Class IIa HDAC inhibitor TMP195 alleviates lipopolysaccharide-induced acute kidney injury[J]. American Journal of Physiology-Renal Physiology, 2020, 319(6): F1015-F1026.
[7] Guerriero J L, Sotayo A, Ponichtera H E, et al. Class IIa HDAC inhibition reduces breast tumours and metastases through anti-tumour macrophages[J]. Nature, 2017, 543(7645): 428-432.
| Cell experiment [1]: | |
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Cell lines |
H460 cells |
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Preparation Method |
H460 cells were cultivated in DMEM medium supplemented with 10% heat-inactivated fetal bovine serum (FBS), 1% penicillin-streptomycin at 37°C in an incubator with 5% CO2. Cells were seeded in a 96-well plate at a density of 1×103 cells/well for 24h. Cells were treated with TMP195 (0, 1, 10, and 100μM), and after different periods (24, 48, and 72h) of treatment, the cell viability was determined. |
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Reaction Conditions |
25μM; 24, 48, and 72h |
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Applications |
TMP195 treatment inhibited the cell viability of H460 cells in a time-dependent manner. |
| Animal experiment [2]: | |
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Animal models |
Male C57BL/6J mice |
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Preparation Method |
Male C57BL/6J mice (6 weeks old; 20-25g) were housed in specific pathogen-free facilities under a 12h light-dark cycle at a temperature of 24±1°C with controlled humidity, and had access to food and water. Mice were engrafted with MC38 colon carcinoma cells in the back of the right hindlimb by subcutaneously injecting 1×106 cells in a 100μl suspension. On the fifth day after MC38 cells were inoculated, the tumor-bearing mice were randomly divided and treated intraperitoneally with 50mg/kg/day TMP195 dissolved in DMSO or an equal volume of DMSO as the control group. Approximately 20 days after subcutaneous inoculation, the mice were sacrificed, and tumors were harvested for analysis. |
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Dosage form |
50mg/kg/day; 15 days; i.p. |
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Applications |
TMP195 treatment reduced the weight and volume of MC38-transplanted tumors in C57BL/6 mice. |
References: [1] Park J, Chen Y Y, Cao J J, et al. MYC plus class IIa HDAC inhibition drives mitochondrial dysfunction in non-small cell lung cancer[J]. Cell Reports, 2025, 44(6). [2] Han Y, Sun J, Yang Y, et al. TMP195 exerts antitumor effects on colorectal cancer by promoting M1 macrophages polarization[J]. International journal of biological sciences, 2022, 18(15): 5653. | |
| Cas No. | 1314891-22-9 | SDF | |
| Canonical SMILES | O=C(NCC(C)(C)C1=COC(C2=CC=CC=C2)=N1)C3=CC(C4=NOC(C(F)(F)F)=N4)=CC=C3 | ||
| Formula | C23H19F3N4O3 | M.Wt | 456.42 |
| الذوبان | DMSO : ≥ 100 mg/mL (219.10 mM);Water : < 0.1 mg/mL (insoluble) | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.191 mL | 10.9548 mL | 21.9096 mL |
| 5 mM | 438.2 μL | 2.191 mL | 4.3819 mL |
| 10 mM | 219.1 μL | 1.0955 mL | 2.191 mL |
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 19 reference(s) in Google Scholar.)