Art. -Nr.: HY-163943

UNI418

Name: UNI418
Brand: MedChemExpress
SKU: HY-163943
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UNI418 is an orally active and potent PIKfyve and PIP5K1C inhibitor with K_d values of 0.78 and 61 nM, respectively. UNI418 exhibits anti-SARS-CoV-2 activity with an EC₅₀ of 1.4 μM. UNI418, through inhibition of PIKfyve and PIP5K1C (IC₅₀ = 60.1 nM), on one hand reduces IP6 levels to trigger Cul4A-WDR5-dependent homologous recombination protein degradation, and on the other hand impairs endolysosomal acidification, cathepsin L maturation, and ACE2-mediated endocytosis, thereby blocking SARS-CoV-2 entry and escape. UNI418 can be used for research on ovarian cancer and SARS-CoV-2 infection.

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Reinheit : 99.61%
CAS. Nr.: 1802068-51-4
Formel: C₂₂H₁₆N₆
Molecular Weight:364.40

Speicherung:

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

UNI418 Chemical Structure

CAS. Nr.: 1802068-51-4

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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
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[2]

PIP5K1C

61 nM (Kd)

PIP5K1C

60.1 nM (IC₅₀)

PIP5K1B

60.7 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	1.65 μM	Cytotoxicity against human HCT116 cells assessed as viability reduction after 72 hrs incubation by CellTiter-Glo assay. Cytotoxicity against human HCT116 cells assessed as viability reduction after 72 hrs incubation by CellTiter-Glo assay.	41935081
HCT-116	IC₅₀	0.44 μM	Cytotoxicity against human HCT116 PARP1−/− cells assessed as viability reduction after 72 hrs incubation by CellTiter-Glo assay. Cytotoxicity against human HCT116 PARP1−/− cells assessed as viability reduction after 72 hrs incubation by CellTiter-Glo assay.	41935081
Vero	EC₅₀	1.4 μM	Antiviral activity against SARS-CoV-2 in Vero cells assessed by immunofluorescence counting of spike-positive cells 2 days postinfection. Antiviral activity against SARS-CoV-2 in Vero cells assessed by immunofluorescence counting of spike-positive cells 2 days postinfection.	39085352
Vero	CC₅₀	62.3 μM	Cytotoxicity against Vero cells assessed by MTT assay 2 days postinfection. Cytotoxicity against Vero cells assessed by MTT assay 2 days postinfection.	39085352
PEO1	IC₅₀	6.83 μM	Clonogenic survival inhibition against PEO-1 cells by UNI418 assessed by methylene blue staining. Clonogenic survival inhibition against PEO-1 cells by UNI418 assessed by methylene blue staining.	41935081
LNCaP C4-2	IC₅₀	4.44 μM	Clonogenic survival inhibition against C4-2 cells by UNI418 assessed by methylene blue staining. Clonogenic survival inhibition against C4-2 cells by UNI418 assessed by methylene blue staining.	41935081
CAPAN-1	IC₅₀	18.20 μM	Clonogenic survival inhibition against Capan-1 cells by UNI418 assessed by methylene blue staining. Clonogenic survival inhibition against Capan-1 cells by UNI418 assessed by methylene blue staining.	41935081

In Vitro

UNI418 (0.5 μM; 18 h) induces degradation of homologous recombination proteins (RAD51, CHK1, and CtIP) in RPE1 and HCT116 cells^[1].
UNI418 (up to 5 μM; 72 h) selectively kills PARP1-deficient HCT116 cells with an IC₅₀ of 0.44 μM versus 1.65 μM in WT cells, and acts synergistically with Olaparib (HY-10162)^[1].
UNI418 shows stronger inhibitory activity against HCT116 PARP1-/- (IC₅₀ = 0.44 μM) than against HCT116 WT (IC₅₀ = 1.65 μM), with IC₅₀ values of 4.44 μM, 5.39 μM, 6.83 μM, and 18.20 μM in C4-2, C2-2, PEO-1, and Capan-1 cells, respectively.^[1]
UNI418 (0.5 μM-1 μM; 2 h) induces SQSTM1/p62 and LC3-II accumulation in RPE1 cells and significantly inhibits autophagic flux^[2].
UNI418 (0.005-100 μM; 2 days) inhibits SARS-CoV-2 infection in Vero cells with an EC₅₀ of 1.4 μM and a CC₅₀ of 62.3 μM (selectivity index 45.6)^[2].
UNI418 (0.001-10 μM; 24 h) significantly reduces viral genome copy numbers in the supernatant and decreases intracellular viral nucleocapsid protein (NP) expression in Vero cells infected with SARS-CoV-2 (MOI 0.001)^[2].
UNI418 (0.125-0.5 μM; pretreatment for 1 h, observation for 24 h) significantly inhibits the entry of Wuhan-Hu-1, Delta, and Omicron variant spike pseudoviruses in 293T-ACE2 cells^[2].
UNI418 (0.5 μM; 30 min pretreatment, 2 h observation after treatment) successfully inhibits spike-RBD-induced ACE2-mediated endocytosis in hACE2-GFP-transfected HEK293T cells^[2].
UNI418 (0.01-10 μM; 1-3 h post-infection) dose-dependently inhibits the reduction of endogenous full-length ACE2 caused by viral infection in SARS-CoV-2-infected Vero cells^[2].
UNI418 (1 h) directly binds to and inhibits PIKfyve and PIP5K1C, with K_D values of 0.74 nM and 61 nM, respectively^[1].
UNI418 (0.25-5 μM; 24 h) inhibits the DNA replication stress response in HEK293T Luc-ATAD5 cells^[1].
UNI418 promotes the protein degradation of RAD51, CHK1, and CtIP without altering their mRNA levels^[1].
UNI418 exhibits inhibitory activity against PIKfyve (K_d = 0.78 nM), PIP5K1C (K_d = 61 nM, IC₅₀ = 60.1 nM), and PIP5K1B (IC₅₀ = 60.7 nM) in in vitro cell-free kinase assays^[2].
UNI418 (1 μM; 1 h) inhibits endosomal/lysosomal acidification and induces vacuolization in Vero cells^[2].
UNI418 (0.5-10 μM) inhibits cathepsin D (Cathepsin D) and cathepsin L (Cathepsin L) proteolytic maturation in Vero81/Vero cells^[2].

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

Western Blot Analysis^[2]

Cell Line:

RPE1 cells
Concentration:

0.5, 1 μM
Incubation Time:

2 h
Result:

Strongly induced the accumulation of SQSTM1/p62 and LC3-II, and markedly inhibited autophagic flux under both normal and starvation conditions

Cell Autophagy Assay^[2]

Cell Line:

stable mCherry-GFP-LC3 expressing HEK293T cells
Concentration:

0.5 μM
Incubation Time:

1, 3, 6 h
Result:

Considerably increased the number of nonacidic autophagosomes (yellow fluorescence), suggesting inhibition of autophagosome-lysosome fusion or lysosomal acidification.

Western Blot Analysis^[2]

Cell Line:

Vero81/Vero cells
Concentration:

0.5, 1, 10 μM
Incubation Time:

4 h
Result:

Inhibited the proteolytic maturation of both cathepsin D and cathepsin L, and largely reduced the lysosomal targeting of cathepsin D (LAMP1 colocalization).

Real Time qPCR^[2]

Cell Line:

Vero cells
Concentration:

0.001, 0.01, 0.1, 1, 10 μM
Incubation Time:

24 hours postinfection
Result:

Drastically reduced the viral genome copies in culture supernatants (by an approximately 2-log reduction at 10 μM).

Western Blot Analysis^[1]

Cell Line:

RPE1 and HCT116 cells
Concentration:

0.5 μM
Incubation Time:

18 h
Result:

Significantly reduced the protein levels of RAD51, CHK1, and CtIP in both soluble and chromatin-bound fractions without affecting their mRNA levels; promoted Cul4A-dependent proteasomal degradation.

Parmacokinetics

Species	Dose	Route	T_1/2	AUC_0-t	CL	V_ss	T_max	C_max	F
Mice^[3]	2 mg/kg	i.v.	0.226 h	260.38 μg·h/mL	0.04 L/h/kg	0.3 L/kg	/	/	/
Mice^[3]	5 mg/kg	p.o.	7.43 h	79.1 μg·h/mL	/	/	0.185 h	0.05 μg/mL	30.38 %

In Vivo

UNI418 (10 mg/kg; s.c.; once every other day; treatment duration 12 days) selectively inhibits the growth of PARP1-deficient tumors and synergizes with Olaparib to inhibit the growth of wild-type tumors in NOD.CB17-Prkdcscid/J mice subcutaneously inoculated with HCT116 WT or PARP1-/- xenograft tumor models^[1].

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

Animal Model:

NOD.CB17-Prkdcscid/J (male, 6 weeks old) were subcutaneously injected with HCT116 WT or PARP1-/- colon cancer cellsinto the right flank^[1]
Dosage:

10 mg/kg
Administration:

s.c.; once every other day; 12 days
Result:

Markedly suppressed tumor growth exclusively in the PARP1-/- xenografts, with no significant effect observed in the WT tumors.
Resulted in the significant inhibition of HCT116 WT tumor growth when co-administered with Olaparib (50 mg/kg), demonstrating an in vivo synergistic effect.
Caused no significant alteration in the body weights of the mice throughout the treatment period, either alone or in combination, indicating good tolerability.

Related Protocols :

Chemical Information

CAS. Nr. 1802068-51-4
Appearance Solid
Molecular Weight 364.40
Formel C₂₂H₁₆N₆
Color Off-white to light brown
SMILES

C1(C2=CC=NC=C2)=NC(NC3=NNC(C4=CC=CC=C4)=C3)=C5C=CC=CC5=N1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (137.21 mM; ultrasonic and warming and heat to 60°C; 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

2.7442 mL

13.7212 mL

27.4424 mL

5 mM

0.5488 mL

2.7442 mL

5.4885 mL

10 mM

0.2744 mL

1.3721 mL

2.7442 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 (301 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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]. Lee SG, et al. Targeting IP signaling to destabilize homologous recombination proteins to overcome PARP inhibitor resistance. Nature communications. 2026 Apr 04;17(1):4871.

[2]. Seo Y, et al. A dual inhibitor of PIP5K1C and PIKfyve prevents SARS-CoV-2 entry into cells. Experimental & molecular medicine. 2024 Aug;56(8):1736-1749. [Content Brief]

[3]. Salisch F, et al. Behind the membranous curtain-lipid dynamics and functions in coronaviral replication. Journal of virology. 2026 May 19;100(5):e0175325.

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	2.7442 mL	13.7212 mL	27.4424 mL	68.6059 mL
	5 mM	0.5488 mL	2.7442 mL	5.4885 mL	13.7212 mL
	10 mM	0.2744 mL	1.3721 mL	2.7442 mL	6.8606 mL
	15 mM	0.1829 mL	0.9147 mL	1.8295 mL	4.5737 mL
	20 mM	0.1372 mL	0.6861 mL	1.3721 mL	3.4303 mL
	25 mM	0.1098 mL	0.5488 mL	1.0977 mL	2.7442 mL
	30 mM	0.0915 mL	0.4574 mL	0.9147 mL	2.2869 mL
	40 mM	0.0686 mL	0.3430 mL	0.6861 mL	1.7151 mL
	50 mM	0.0549 mL	0.2744 mL	0.5488 mL	1.3721 mL
	60 mM	0.0457 mL	0.2287 mL	0.4574 mL	1.1434 mL
	80 mM	0.0343 mL	0.1715 mL	0.3430 mL	0.8576 mL
	100 mM	0.0274 mL	0.1372 mL	0.2744 mL	0.6861 mL

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UNI418