Art. -Nr.: HY-178360

NP1192

Name: NP1192
Brand: MedChemExpress
SKU: HY-178360
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NP1192 is a potent, selective PROTAC NAT10 degrader. NP1192 promotes NAT10 ubiquitination and degradation. NP1192 inhibits ac4C modification. NP1192 demonstrates dual inhibition of hypoxia-driven glycolysis and immunosuppression via NAT10/HIF-1α/PD-L1 axis disruption, achieving superior antitumor efficacy and synergizing with anti-PD-L1 both in vitro and in vivo. NP1192 can be used for ovarian, cervical, and glioblastoma cancer research.
(Pink: NAT10 ligand (HY-16706); Blue: Cereblon ligand (HY-148834); Black: linker).

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Reinheit: 99.02%
CAS. Nr.: 2966791-41-1
Formel: C₃₉H₄₂N₈O₅S
Molecular Weight:734.87

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

NP1192 Chemical Structure

CAS. Nr.: 2966791-41-1

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

NP1192 is a potent, selective PROTAC NAT10 degrader. NP1192 promotes NAT10 ubiquitination and degradation. NP1192 inhibits ac4C modification. NP1192 demonstrates dual inhibition of hypoxia-driven glycolysis and immunosuppression via NAT10/HIF-1α/PD-L1 axis disruption, achieving superior antitumor efficacy and synergizing with anti-PD-L1 both in vitro and in vivo. NP1192 can be used for ovarian, cervical, and glioblastoma cancer research^[1]^[2]^[3]. (Pink: NAT10 ligand (HY-16706); Blue: Cereblon ligand (HY-148834); Black: linker).

IC₅₀ & Target^[1]

NAT10

HIF-1α

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle Histone Acetyltransferase Isoform-spezifische Produkte anzeigen :

Alle HIF/HIF Prolyl-Hydroxylase Isoform-spezifische Produkte anzeigen :

In Vitro

NP1192 (0-20 μM, 24-48 h) induces NAT10 degradation in SiHa (human) and U14 (murine) CCa cell lines in a dose-and time-dependent manner, through the ubiquitin-proteasome system (UPS) rather than via lysosomal pathways^[1].
NP1192 (36 h) inhibits cervical cancer (SiHa) cell growth with an IC₅₀ of 7.814 μM (76.2 μM in resistant cells) and additionally shows dose-dependent efficacy in organoids, with IC₅₀ values of 9.947, 3.048, and 13.76 μM for ovarian (OV), cervical (CESC), and glioblastoma (GBM) models, respectively^[1].
NP1192 (20 μM, 0-72 h and 2 weeks) significantly reduces cell viability, induces cell cycle arrest, and suppresses invasion and clonogenic growth in CCa cells^[1].
NP1192 (0.195-50 μM, 1-8 days) induces a pronounced reduction in organoid size and number across tumor models (ovarian, cervical, and glioblastoma), while the corresponding normal organoids remained unaltered, indicating minimal cytotoxicity to nonmalignant tissues^[1].
NP1192 (20 μM, 36 h) reprograms the hypoxic tumor microenvironment (TME) and metabolism in CCa cells by degrading NAT10 and thereby impairing HIF-1α expression, which disrupts glycolysis as evidenced by reduced glucose uptake and lactate production alongside elevated ATP levels^[1].

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

Western Blot Analysis^[1]

Cell Line:

SiHa, U14, and HFF-1 cells
Concentration:

0, 1.25, 2.5, 5, 10 and 20 μM
Incubation Time:

24, 36 and 48 h
Result:

Led to a substantial depletion of total NAT10 protein in SiHa (human) and U14 (murine) CCa cell lines in a a dose-and time-dependent manner.
Induced degradation rates of 28%, 32%, 40%, and 43% in SiHa cells at concentrations of 1.25, 2.5, 5, and 10 μM, respectively, with a maximum of 69% degradation at 20 μM after 36 h and only 20% degradation after 24 h.
Led to a nearly 70% reduction in the NAT10 protein content in murine U14 cervical cells after 36 h.
Did not exhibit the classical hook effect even at concentrations as high as 20 μM.
Failed to degrade NAT10 significantly when co-treated with MG132 (HY-13259), whereas Bafilomycin A1 (HY-100558) exerted no discernible effect on its degradation efficacy.
Substantially induced minimal cytotoxicity in nonmalignant HFF-1 cells with low NAT10 expression.
Decreased HIF-1α protein levels.
Reversed the induction of hypoxia-related genes under hypoxic conditions, such as HIF1A and PD-L1, at both mRNA and protein levels.

Cell Proliferation Assay^[1]

Cell Line:

SiHa cells and NAT10-KD SiHa cells
Concentration:

20 μM
Incubation Time:

2 weeks
Result:

Led to a substantial decrease in colony formation capacity, with the magnitude of inhibition being only second to that in NAT10-knockdown cells.

Cell Invasion Assay^[1]

Cell Line:

SiHa cells and NAT10-KD SiHa cells
Concentration:

20 μM
Incubation Time:

36 h
Result:

Substantially hindered cell invasion with a significant decrease in the number of cells crossing the basement membrane.

Parmacokinetics

Species	Dose	Route	Note	AUC_0-t	AUC_0-∞	MRT_0-t	MRT_0-∞	T_1/2	T_max	C_max	F	CL	V_z
Rat^[1]	10 mg/kg	p.o.	Male SD Rats	24.7 ng·h/mL	29.5 ng·h/mL	1.56 h	2.85 h	2.40 h	1.67 h	13.9 ng/mL	1.35 %	/	/
Rat^[1]	2 mg/kg	i.v.	Male SD Rats	365 ng·h/mL	367 ng·h/mL	0.529 h	0.570 h	0.967 h	0.0833 h	759 ng/mL	/	5.503 L/h/kg	7.597 L/kg

In Vivo

NP1192 (25 mg/kg, i.p., every 2 days for a week) synergizes with anti-PD-L1 to inhibit tumor growth, suppress glycolysis, and enhance CD8⁺ T_eff cell immunity in U14-luc xenograft mouse model^[1].

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

Animal Model:

Female C57BL/6J mice (6-8 weeks old) subcutaneously injected with U14-luc cells^[1]
Dosage:

25 mg/kg
Administration:

i.p., every 2 days for a week
Result:

Significantly reduced tumor volume and tumor burden compared to DMSO at 25 mg/kg.
Significantly inhibited tumor growth when combined with anti-PD-L1 antibody (2.5 mg/kg).
Showed the most pronounced reduction (>80%) in tumor lactate levels when combined with anti-PD-L1 antibody (2.5 mg/kg).
¹⁸F-FDG PET–CT imaging revealed minimal metabolic uptake when combined with anti-PD-L1 antibody, suggesting effective suppresses tumor metabolic activity.
Enhanced the CD8⁺ T_eff cell population, reprograms the TME, and potentiates antitumor immunity when combined with anti-PD-L1 blockade.
Did not cause significant weight loss or systemic toxicity both alone and in combination.

Chemical Information

CAS. Nr. 2966791-41-1
Appearance Solid
Molecular Weight 734.87
Formel C₃₉H₄₂N₈O₅S
SMILES

N#CC1=CC=C(C=C1)C2=CSC(N(/N=C3CCCC/3)CCCCCCC(N4CCN(CC4)C5=C6C(N(C(C6=CC=C5)=O)C7CCC(NC7=O)=O)=O)=O)=N2
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (136.08 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

1.3608 mL

6.8039 mL

13.6078 mL

5 mM

0.2722 mL

1.3608 mL

2.7216 mL

10 mM

0.1361 mL

0.6804 mL

1.3608 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

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

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (289 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]. Ao, K., et al. Targeted NAT10 Degradation by PROTAC NP1192 Suppresses Hypoxia-Adaptive Glycolysis and Reinvigorates CD8+ Effector T-Cell Function for Synergistic Cancer Immunotherapy. ACS Central Science. 2025.

[2]. Zhou Q, et al. PROTAC technology for sensitizing melanoma to immune checkpoint therapy[J]. Journal of Experimental & Clinical Cancer Research, 2026.

[3]. Xiong J, et al. Functional roles and mechanisms of NAT10-mediated RNA ac4C modification in normal development and cancer progression. Front Cell Dev Biol. 2026 Mar 6;14:1795359.

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, 6 months; -20°C, 1 month. 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	1.3608 mL	6.8039 mL	13.6078 mL	34.0196 mL
	5 mM	0.2722 mL	1.3608 mL	2.7216 mL	6.8039 mL
	10 mM	0.1361 mL	0.6804 mL	1.3608 mL	3.4020 mL
	15 mM	0.0907 mL	0.4536 mL	0.9072 mL	2.2680 mL
	20 mM	0.0680 mL	0.3402 mL	0.6804 mL	1.7010 mL
	25 mM	0.0544 mL	0.2722 mL	0.5443 mL	1.3608 mL
	30 mM	0.0454 mL	0.2268 mL	0.4536 mL	1.1340 mL
	40 mM	0.0340 mL	0.1701 mL	0.3402 mL	0.8505 mL
	50 mM	0.0272 mL	0.1361 mL	0.2722 mL	0.6804 mL
	60 mM	0.0227 mL	0.1134 mL	0.2268 mL	0.5670 mL
	80 mM	0.0170 mL	0.0850 mL	0.1701 mL	0.4252 mL
	100 mM	0.0136 mL	0.0680 mL	0.1361 mL	0.3402 mL

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NP1192

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Histone Acetyltransferase Isoform-spezifische Produkte anzeigen

Alle HIF/HIF Prolyl-Hydroxylase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

NP1192 Related Classifications

HY-178360 Related Classifications

Bioz