Cat. No.: HY-159520

Ofirnoflastum

(Synonyms: Ofirnoflast; HT-6184)

고객리뷰

Based on 1 Customer Validation

Ofirnoflastum (Ofirnoflast) is an orally active first-in-class allosteric NEK7 inhibitor with an IC₅₀ of 46 nM. Ofirnoflastum binds an allosteric site adjacent to NEK7’s ATP-binding pocket, induces conformational shifts, disrupts NEK7-NLRP3 binding, blocks NLRP3 inflammasome assembly, spares NEK7’s physiological functions, and suppresses caspase-1, caspase-8, NF-κB, and TNF activity. Ofirnoflastum reduces pro-inflammatory cytokine production, suppresses ASC specks, IL-1β release, pyroptotic cell death, and leukemic burden, induces apoptosis and erythroid differentiation, restores hematopoiesis, and improves outcomes in colitis models. Ofirnoflastum can be used for the research of myelodysplastic syndromes, chronic myelomonocytic leukemia, and acute myeloid leukemia.

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Purity: 99.93%
CAS No.: 2731294-23-6
화학식: C₂₃H₁₉F₄N₇O₂
분자량:501.44

보관:

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

Ofirnoflastum Chemical Structure

CAS No.: 2731294-23-6

사이즈

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
용액&용해도
- In Vitro
- In Vivo
순도&문서
References
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target^[3]^[4]

NEK7

46 nM (IC₅₀)

Caspase 8

Caspase-1

NLRP3

All NEKs Isoforms :

All NOD-like Receptor (NLR) Isoforms :

All Caspase Isoforms :

All NF-κB Isoforms :

In Vitro

Ofirnoflast (range of concentrations; 30 min pre-incubation, 3 h LPS (HY-D1056) priming, 3 h Nigericin (HY-100381) stimulation) inhibits nigericin-induced IL-1β secretion in PMA-differentiated THP-1 macrophages with an IC₅₀ of 198 nM^[3].
Ofirnoflast (range of concentrations; 30 min pre-incubation, 3 h LPS priming, 3 h Nigericin stimulation) prevents nigericin-induced pyroptotic cell death in PMA-differentiated THP-1 macrophages with an EC₅₀ of 378 nM^[3].
Ofirnoflast (0.01-10 μM; 3 h LPS priming, 2 h pre-incubation, 1 h nigericin stimulation) inhibits nigericin-induced ASC speck formation in THP-1-ASC-GFP cells with an IC₅₀ of 0.194 μM^[3].
Ofirnoflast (range of concentrations; 5 h LPS priming, final hour with compound, 30 min nigericin stimulation) inhibits nigericin-induced IL-1β secretion in human iPSC-derived microglia with an IC₅₀ of 44 nM^[3].
Ofirnoflast (1 μM; 5 h LPS priming, final hour with compound, 45 min ATP stimulation) potently inhibits ATP-induced IL-1β secretion in human iPSC-derived microglia^[3].
Ofirnoflastum potently inhibits proinflammatory cytokine secretion, Caspase-1 and Caspase-8 activity, and reverses erythroid differentiation block in LPS-activated inflammatory monocytes, Tet2-mutant monocytes, CMML patient-derived cells, myeloid leukemia cell lines, and MDS patient-derived cells^[4].
Ofirnoflastum's anti-inflammatory effects in myeloid leukemia cells are dependent on NEK7 expression^[4].
Ofirnoflastum's anti-leukemic activity in Tet2-mutant cells and primary MDS/CMML patient-derived cells is mediated through suppression of chronic inflammation driven by the IL-1β/IL1R1 axis^[4].

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

Immunofluorescence^[3]

Cell Line:

THP-1-ASC-GFP cells
Concentration:

0.01-10 μM
Incubation Time:

3 h LPS priming; 2 h pre-incubation; 1 h nigericin stimulation
Result:

Dose-dependently reduced ASC-GFP speck formation, with an IC₅₀ of 0.194 μM.

ELISA Assay^[3]

Cell Line:

Human iPSC-derived microglial cells
Concentration:

1 μM
Incubation Time:

5 h LPS priming (final hour with compound); 45 min ATP stimulation
Result:

Strongly inhibited ATP-induced IL-1β secretion, with levels reduced to near baseline.

Parmacokinetics

Species	Dose	Route	C₀	T_1/2	AUC_last	AUC_inf	CL	V_dss	C_max	T_max	F
Mice^[3]	0.5 mg/kg	i.v.	634.3 ng/mL	1.31 h	530.3 ng·h/mL	537.3 ng·h/mL	15.7 mL/min/kg	1.25 L/kg	/	/	/
Mice^[3]	10 mg/kg	p.o.	/	2.7 h	14280.3 ng·h/mL	16324.8 ng·h/mL	/	/	2684.1 ng/mL	2 h	134.7 %

In Vivo

Ofirnoflastum (1-5 mg/kg; p.o.; twice daily; day 0 through day 7) reduces disease activity, histopathological damage, and inflammatory cytokine levels in a mouse model of DSS (HY-116282C)-induced colitis, with maximal efficacy achieved at the lowest tested dose^[3].
Ofirnoflastum reduces MDS/AML leukemic burden by ~3-fold in patient-derived xenograft mice via suppression of inflammatory/proliferative pathways and induction of apoptosis and erythroid differentiation^[4].
Ofirnoflastum reduces CMML leukemic burden by ~3-fold in patient-derived xenograft mice via suppression of inflammatory/proliferative pathways and induction of apoptosis and erythroid differentiation^[4].

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

Animal Model:

C57BL/6 (female, 11-12 weeks old, 20-25 g, DSS-induced colitis)^[3]
Dosage:

1 mg/kg; 2 mg/kg; 5 mg/kg
Administration:

p.o.; twice daily; day 0 through day 7
Result:

Reduced clinical Disease Activity Index (DAI) scores and histopathological damage, including epithelial degeneration, crypt injury, and immune cell infiltration.
Achieved plasma and colon concentrations exceeding in vitro EC₅₀ values and significantly suppressed inflammasome-dependent cytokines (IL-1β, IL-18) and broader inflammatory markers (IL-6, TNF-α, IFN-γ, CXCL1, MIP1a) in both colon homogenates and plasma.
Did not yield additional benefit at the highest dose (5 mg/kg) and was associated with a slight increase in DAI and histopathology scores.

Chemical Information

CAS No. 2731294-23-6
Appearance Solid
분자량 501.44
화학식 C₂₃H₁₉F₄N₇O₂
Color White to off-white
SMILES

O=C(NC1=C(F)C=C(C2=CN(C3CC3)C4=C2C(N)=NC=N4)C=C1)NC5=NOC(C6(C(F)(F)F)CC6)=C5
Synonyms

Ofirnoflast; HT-6184
선적

Room temperature in continental US; may vary elsewhere.

보관

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

용액&용해도

In Vitro:

DMSO : ≥ 100 mg/mL (199.43 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

1.9943 mL

9.9713 mL

19.9426 mL

5 mM

0.3989 mL

1.9943 mL

3.9885 mL

10 mM

0.1994 mL

0.9971 mL

1.9943 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.

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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: ≥ 2.5 mg/mL (4.99 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (4.99 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (4.99 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals 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

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (286 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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)

References

[1]. Devan Bursey, et al. The novel allosteric NEK7 inhibitor ofirnoflast (HT-6184) suppresses IL-8 and other pro-inflammatory cytokines in patients with low-risk myelodysplastic syndrome and symptomatic anemia. Blood Volume 146, Supplement 1, 3 November 2025, Page 2092.

[2]. Devan Bursey, et al. The novel allosteric NEK7 inhibit ofirnoflast (HT-6184) reduces oxidized mitochondrial DNA in patients with low-risk myelodysplastic syndrome. Blood Volume 146, Supplement 1, 3 November 2025, Page 2093.

[3]. Mollard A, et al. Ofirnoflast: a first-in-class NEK7-targeted inhibitor of the NLRP3 inflammasome. J Drug Target. 2026;34(1):100-112. [Content Brief]

[4]. Divij Verma, et al. Ofirnoflast, a novel inflammasome inhibitor, rewires transcriptional programs and shows clinical and preclinical efficacy in myeloid neoplasms. Blood Volume 146, Supplement 1, 3 November 2025, Page 323.

[5]. Varun Bafna, et al. The novel allosteric NEK7 inhibitor ofirnoflast (HT-6184) demonstrates robust and sustained hematologic response in subjects with IPSS-R very low, low or intermediate risk myelodysplastic syndrome (MDS) and symptomatic anemia. Blood Volume 146, Supplement 1, 3 November 2025, Page 5622.

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	1.9943 mL	9.9713 mL	19.9426 mL	49.8564 mL
	5 mM	0.3989 mL	1.9943 mL	3.9885 mL	9.9713 mL
	10 mM	0.1994 mL	0.9971 mL	1.9943 mL	4.9856 mL
	15 mM	0.1330 mL	0.6648 mL	1.3295 mL	3.3238 mL
	20 mM	0.0997 mL	0.4986 mL	0.9971 mL	2.4928 mL
	25 mM	0.0798 mL	0.3989 mL	0.7977 mL	1.9943 mL
	30 mM	0.0665 mL	0.3324 mL	0.6648 mL	1.6619 mL
	40 mM	0.0499 mL	0.2493 mL	0.4986 mL	1.2464 mL
	50 mM	0.0399 mL	0.1994 mL	0.3989 mL	0.9971 mL
	60 mM	0.0332 mL	0.1662 mL	0.3324 mL	0.8309 mL
	80 mM	0.0249 mL	0.1246 mL	0.2493 mL	0.6232 mL
	100 mM	0.0199 mL	0.0997 mL	0.1994 mL	0.4986 mL

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Ofirnoflastum

MCE Bioactive Compound Library

All NEKs Isoforms

All NOD-like Receptor (NLR) Isoforms

All Caspase Isoforms

All NF-κB Isoforms

Biological Activity

Chemical Information

용액&용해도

순도&문서

References

Help & FAQs

Complete Stock Solution Preparation Table

Ofirnoflastum Related Classifications

HY-159520 Related Classifications