Art. -Nr.: HY-10074

TPCA-1

43 Cited Publications

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Based on 43 publication(s) in Google Scholar

TPCA-1 is a potent and selective inhibitor of IKK-2 with IC₅₀ of 17.9 nM. TPCA-1 is an effective inhibitor of STAT3 phosphorylation, DNA binding, and transactivation.

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Reinheit: 98.75%
CAS. Nr.: 507475-17-4
Formel: C₁₂H₁₀FN₃O₂S
Molecular Weight:279.29

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

TPCA-1 Chemical Structure

CAS. Nr.: 507475-17-4

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (43)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

TPCA-1 is a potent and selective inhibitor of IKK-2 with IC₅₀ of 17.9 nM. TPCA-1 is an effective inhibitor of STAT3 phosphorylation, DNA binding, and transactivation.

IC₅₀ & Target^[3]

IKK-2

17.9 nM (IC₅₀)

STAT3

Alle IKK Isoform-spezifische Produkte anzeigen :

Alle STAT Isoform-spezifische Produkte anzeigen :

In Vitro

TPCA-1 inhibits lipopolysaccharide-induced human monocyte production of TNF-α, IL-6, and IL-8 with an IC₅₀ of 170 to 320 nM^[1]^[2].
TPCA-1 (0-2 μM) inhibits STAT3 phosphorylation and transactivation induced by cytokines and nonreceptor tyrosine kinase in dose- and time-dependent manner. TPCA-1 completely inhibits STAT3 phosphorylation without changing total STAT3 levels^[3].
TPCA-1 increased sensitivity to ZD1839 in both TKI sensitive cells and insensitive cells^[3].

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

Cell Viability Assay^[2]

Cell Line:

human peripheral blood monocytes stimulated with LPS.
Concentration:

0-10 μM.
Incubation Time:

~24 hours.
Result:

TPCA-1 Inhibits LPS-Induced TNF-α, IL-6, and IL-8 production by human monocytes.

Cell Viability Assay^[3]

Cell Line:

HCC827 and H1975 cells.
Concentration:

0-10 μM.
Incubation Time:

0.5-2 hours.
Result:

Suppressed proliferation of HCC827 and H1975 cells.
Led to a G₂-M cell-cycle arrest in HCC827 but not A549.

Western Blot Analysis^[3]

Cell Line:

HEK-293T cell lines.
Concentration:

0-2 μM (before IL-2 or IFN-α treatment).
Incubation Time:

0.5-2 hours.
Result:

Inhibited STAT3 phosphorylation and transactivation induced by cytokines and nonreceptor tyrosine kinase in dose- and time-dependent manner.

In Vivo

TPCA-1 (3, 10, or 20 mg/kg, i.p.) results in a dose-dependent reduction in the severity of murine collagen-induced arthritis (CIA)^[2].
TPCA-1(10 mg/kg, i.p. daily) inhibits growth of NSCLC with EGFR mutation and potentiates antitumor effect of ZD1839 in xenograft models^[3].

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

Animal Model:

10-12 weeks old male DBA/1 OlaHsd mice^[2].
Dosage:

3, 10, or 20 mg/kg.
Administration:

I.P., b.i.d, from days 1 to 47.
Result:

Reduced the severity and delays the onset of CIA.
Attenuated ex vivo antigen-induced T cell proliferation in CIA.

Animal Model:

Six-week-old BALB/c female nude mice injected subcutaneously with HCC827 cells (5×10⁶)^[3].
Dosage:

10 mg/kg.
Administration:

Intraperitoneally daily.
Result:

The tumor weight inhibition rate of TPCA-1, ZD1839, and their combination are 0.419(E_TPCA-1), 0.680(E_ZD1839), and 0.837(E_observed), respectively.

Chemical Information

CAS. Nr. 507475-17-4
Appearance Solid
Molecular Weight 279.29
Formel C₁₂H₁₀FN₃O₂S
Color White to gray
SMILES

O=C(C1=C(NC(N)=O)SC(C2=CC=C(F)C=C2)=C1)N
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (43)

All WBCell Proliferation/Viability Assay

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Journal Impact Factor

Signal Transduct Target Ther

RNA-induced liquid phase separation of SARS-CoV-2 nucleocapsid protein facilitates NF-κB hyper-activation and inflammation. [Abstract]

2021 Apr 24;6(1):167. PMID: 33895773
Cancer Cell

2026 May 21:S1535-6108(26)00220-5. PMID: 42167227
Cancer Cell

Putting the STING back into BH3-mimetic drugs for TP53-mutant blood cancers. [Abstract]

2024 May 13;42(5):850-868.e9. PMID: 38670091

TPCA-1 purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2024 May 13;42(5):850-868.e9. [Abstract]

Cell viability assays of Eμ-Myc lymphoma cell lines treated with ADU-S100 (HY-12885A; AH15A/560: 0.5 μg/mL; 47A: 5 μg/mL) and/or TPCA-1 (HY-10074) for 24 h. Error bars represent SD for three independent experiments. Diagram illustrates how TPCA-1 acts to inhibit NF-κB signaling.
Cell Stem Cell

Bacterial ADP-heptose triggers stem cell regeneration in the intestinal epithelium following injury. [Abstract]

2025 Aug 7;32(8):1235-1250.e6. PMID: 40651470
Cell Mol Immunol

cFLIPS regulates alternative NLRP3 inflammasome activation in human monocytes. [Abstract]

2023 Oct;20(10):1203-1215. PMID: 37591930
ACS Nano

Neutrophil-Mediated Delivery of Therapeutic Nanoparticles across Blood Vessel Barrier for Treatment of Inflammation and Infection. [Abstract]

2015 Dec 22;9(12):11800-11. PMID: 26516654

TPCA-1 purchased from MedChemExpress. Usage Cited in: ACS Nano. 2015 Dec 22;9(12):11800-11. [Abstract]

Neutrophil-mediated delivery of TPCA-1 mitigates acute lung inflammation/injury. Numbers of leukocytes and neutrophils, concentrations of IL-6 in BALF 20 h after iv injection of vehicle of TPCA-1 solution, 5% glucose, TPCA-1 solution or TPAC-1 BSA NPs in mice 4 h after LPS challenge (8 mg/kg).
Nat Commun

Small round cell sarcoma tumoroid biobank reveals CIC::DUX4 sarcoma vulnerability to MCL-1 inhibition. [Abstract]

2025 Aug 21;16(1):7689. PMID: 40841360
Nat Commun

Dual rectification of metabolism abnormality in pancreatic cancer by a programmed nanomedicine. [Abstract]

2024 Dec 3;15(1):10526. PMID: 39627234
Nat Commun

FGFR inhibition blocks NF-ĸB-dependent glucose metabolism and confers metabolic vulnerabilities in cholangiocarcinoma. [Abstract]

2024 May 7;15(1):3805. PMID: 38714664
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
J Clin Invest

IL-17-producing γδ T cells in the tumor microenvironment promote radioresistance in mice. [Abstract]

2025 Oct 7:e193945. PMID: 41055972
Pharmacol Res

CCL22 signaling contributes to sorafenib resistance in hepatitis B virus-associated hepatocellular carcinoma. [Abstract]

2020 Jul;157:104800. PMID: 32278046
Cell Death Dis

Quantitative analysis of phosphoproteome in necroptosis reveals a role of TRIM28 phosphorylation in promoting necroptosis-induced cytokine production. [Abstract]

2021 Oct 23;12(11):994. PMID: 34689152
Cell Death Dis

Necroptosis promotes cell-autonomous activation of proinflammatory cytokine gene expression. [Abstract]

2018 Apr 27;9(5):500. PMID: 29703889

TPCA-1 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2018 Apr 27;9(5):500. [Abstract]

Western blotting analysis of lysates from 3×HA-IκBα-expressing HT-29 cells treated as indicated for 8 h.
Cell Death Dis

Distinct outcomes of CRL-Nedd8 pathway inhibition reveal cancer cell plasticity. [Abstract]

2016 Dec 1;7(12):e2505. PMID: 27906189
Proc Natl Acad Sci U S A

Chaperone-mediated autophagy is involved in the execution of ferroptosis. [Abstract]

2019 Feb 19;116(8):2996-3005. PMID: 30718432

TPCA-1 purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2019 Feb 19;116(8):2996-3005. [Abstract]

HT22 cells were pretreated with the indicated inhibitors (CDDO (Bardoxolone, HY-14909); T0070907 (HY-13202); Troglitazone (HY-50935 ); TPCA-1 (HY-10074); JAKi; STAT3i; AV-412 (HY-10346); and MK2206 (HY-10358)) and then treated with T/Z, T/S/Z, T/C/Z for 9 h or Glutamate, Erastin (T: 20 ng/ml; Z: 50 μM; S: 20 nM; C: 1 μg/ml; Glutamate: 50 mM; Erastin 10 μM) for 12 h. Cell viability was measured by CellTiterGlo assay.
Cell Death Discov

RIPK1 S213E mutant suppresses RIPK1-dependent cell death by preventing interactions with RIPK3 and CASP8. [Abstract]

2025 Jul 25;11(1):345. PMID: 40715038
Cell Rep

Oxidized mC modulates synthetic lethality to PARP inhibitors for the treatment of leukemia. [Abstract]

2023 Jan 31;42(1):112027. PMID: 36848231
Anal Chem

Metal-Enhanced Aggregation-Induced Emission Strategy for the HIV-I RNA-Binding Ligand Assay. [Abstract]

2022 Mar 22;94(11):4695-4702. PMID: 35258935
Sci Signal

Protein phosphatase 6 activates NF-κB to confer sensitivity to MAPK pathway inhibitors in KRAS- and BRAF-mutant cancer cells. [Abstract]

2024 May 14;17(836):eadd5073. PMID: 38743809
Cancer Cell Int

Construction of a prognostic model with histone modification-related genes and identification of potential drugs in pancreatic cancer. [Abstract]

2021 Jun 5;21(1):291. PMID: 34090418
Int J Mol Med

Transcriptome‑based drug repositioning identifies TPCA‑1 as a potential selective inhibitor of esophagus squamous carcinoma cell viability. [Abstract]

2022 Jun;49(6):75. PMID: 35417037
J Invest Dermatol

Advanced Glycation End Products Promote Melanogenesis by Activating NLRP3 Inflammasome in Human Dermal Fibroblasts. [Abstract]

2022 Oct;142(10):2591-2602.e8. PMID: 35421403
Pharmaceutics

Enhancing the Treatment of Uncontrolled Inflammation through the Targeted Delivery of TPCA-1-Loaded Nanoparticles. [Abstract]

2023 Oct 9;15(10):2435. PMID: 37896195
Inflamm Res

Lactate acts as a metabolic brake on inflammation by repressing NLRP3 transcription via NF-κB inhibition. [Abstract]

2026 Jun 11;75(1):137. PMID: 42274732
Inflammation

Sodium Houttuyfonate Ameliorates DSS-induced Colitis Aggravated by Candida albicans through Dectin-1/NF-κB/miR-32-5p/NFKBIZ Axis Based on Intestinal microRNA Profiling. [Abstract]

2025 Apr;48(2):820-838. PMID: 38963571
Biol Direct

PNSC928, a plant-derived compound, specifically disrupts CtBP2-p300 interaction and reduces inflammation in mice with acute respiratory distress syndrome. [Abstract]

2024 Jun 21;19(1):48. PMID: 38902802
Int J Mol Sci

Dual Role of Interleukin-20 in Different Stages of Osteoclast Differentiation and Its Osteoimmune Regulation during Alveolar Bone Remodeling. [Abstract]

2023 Feb 14;24(4):3810. PMID: 36835229
Int Immunopharmacol

IL-8 promotes lens capsular residual cells migration by down-regulates expression of E-cadherin and ZO-1 via the CXCR1/2-NF-κB-RhoA signal pathway. [Abstract]

2024 Sep 7;142(Pt A):113074. PMID: 39244903
Inflamm Bowel Dis

Pro-inflammatory Cytokines Promote the Occurrence and Development of Colitis-associated Colorectal Cancer by Inhibiting miR-615-5p. [Abstract]

2023 Jun 10;izad105. PMID: 37300504
J Biotechnol

Interferon inhibitors increase rAAV production in HEK293 cells. [Abstract]

2025 Mar:399:9-18. PMID: 39824361
Aging (Albany NY)

HSP90 acts as a senomorphic target in senescent retinal pigmental epithelial cells. [Abstract]

2021 Sep 8;13(17):21547-21570. PMID: 34495872
Cell Signal

Ubiquitin-editing enzyme A20 protects the inflammatory injury of human corneal epithelial cells against lipoteichoic acid. [Abstract]

2025 Jun 25:111962. PMID: 40578588
Exp Cell Res

Continuous NF-κB pathway inhibition promotes expansion of human phenotypical hematopoietic stem/progenitor cells through metabolism regulation. [Abstract]

2021 Feb 15;399(2):112468. PMID: 33428903
J Sci Food Agric

Ginkgo biloba sarcotesta polysaccharide inhibits inflammatory responses through suppressing both NF-κB and MAPK signaling pathway. [Abstract]

2019 Mar 30;99(5):2329-2339. PMID: 30338529
J Immunol

Complex Regulation Pattern of IRF3 Activation Revealed by a Novel Dimerization Reporter System. [Abstract]

2016 May 15;196(10):4322-30. PMID: 27045107

TPCA-1 purchased from MedChemExpress. Usage Cited in: J Immunol. 2016 May 15;196(10):4322-30. [Abstract]

HEK293T (IRF3-BiLC) cells are pretreated with TPCA-1 for 1 h, stimulated with TNF-α for 12 h, and then transfected with poly(I:C) for 12 h, after which IRF3-BiLC luciferase activity is measured.
PLoS One

Interleukin-1β triggers matrix metalloprotease-3 expression through p65/RelA activation in melanoma cells. [Abstract]

2022 Nov 29;17(11):e0278220. PMID: 36445856
bioRxiv

2026 Mar 31.
Res Sq

2026 Jan 9.
University of Toronto

2025.
University of Bonn

2025.
SSRN

2023 Jun 29.
SSRN

2023 Jul 10.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 100 mg/mL (358.05 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.5805 mL

17.9025 mL

35.8051 mL

5 mM

0.7161 mL

3.5805 mL

7.1610 mL

10 mM

0.3581 mL

1.7903 mL

3.5805 mL

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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molaritätsrechner

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

Mass

Konzentration

Volumen

Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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: ≥ 7.5 mg/mL (26.85 mM); Clear solution

This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 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.

Protocol 2

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

Solubility: ≥ 7.5 mg/mL (26.85 mM); Clear solution

This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 7.5 mg/mL (26.85 mM); Clear solution

This protocol yields a clear solution of ≥ 7.5 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 (75.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Sachse F, et al. IKK-2 inhibitor TPCA-1 represses nasal epithelial inflammation in vitro.Rhinology. 2011 Jun;49(2):168-73. [Content Brief]

[2]. Podolin PL, et al. Attenuation of murine collagen-induced arthritis by a novel, potent, selective small molecule inhibitor of IkappaB Kinase 2, TPCA-1 (2-[(aminocarbonyl)amino]-5-(4-fluorophenyl)-3-thiophenecarboxamide), occurs via reduction of proinflamm [Content Brief]

[3]. Nan J, et al. TPCA-1 is a direct dual inhibitor of STAT3 and NF-κB and regresses mutant EGFR-associated human non-small cell lung cancers. Mol Cancer Ther. 2014 Mar;13(3):617-29. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.5805 mL	17.9025 mL	35.8051 mL	89.5127 mL
	5 mM	0.7161 mL	3.5805 mL	7.1610 mL	17.9025 mL
	10 mM	0.3581 mL	1.7903 mL	3.5805 mL	8.9513 mL
	15 mM	0.2387 mL	1.1935 mL	2.3870 mL	5.9675 mL
	20 mM	0.1790 mL	0.8951 mL	1.7903 mL	4.4756 mL
	25 mM	0.1432 mL	0.7161 mL	1.4322 mL	3.5805 mL
	30 mM	0.1194 mL	0.5968 mL	1.1935 mL	2.9838 mL
	40 mM	0.0895 mL	0.4476 mL	0.8951 mL	2.2378 mL
	50 mM	0.0716 mL	0.3581 mL	0.7161 mL	1.7903 mL
	60 mM	0.0597 mL	0.2984 mL	0.5968 mL	1.4919 mL
	80 mM	0.0448 mL	0.2238 mL	0.4476 mL	1.1189 mL
	100 mM	0.0358 mL	0.1790 mL	0.3581 mL	0.8951 mL

Keywords

TPCA-1

43 Cited Publications

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TPCA-1

Apoptosis Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

NF-κB Signaling Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

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Anti-Aging Compound Library

Differentiation Inducing Compound Library

Anti-Breast Cancer Compound Library

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Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Obesity Compound Library

Transcription Factor-Targeted Library

Anti-Liver Cancer Compound Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Kinase Inhibitor Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) TPCA-1

Alle IKK Isoform-spezifische Produkte anzeigen

Alle STAT Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (43)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

TPCA-1 Related Classifications

Art. -Nr.: HY-10074