2. Immunology/Inflammation
  3. NOD-like Receptor (NLR)
  4. BAL-1516

BAL-1516 is an orally active NLRP3 inhibitor with human NLRP3 Kd of 14.2 nM, mouse NLRP3 Kd of 200 nM, and blood-brain barrier penetration.BAL-1516 binds to a surface groove of the NLRP3 nucleotide-binding domain, contacts FISNA and WHD subdomains, forms three hydrogen bonds to the peripheral β-strand of the triple-ATPase, and does not alter NLRP3 ATP-hydrolysis activity.BAL-1516 shows specificity for NLRP3 over other NOD-like receptors, directly binds mouse NLRP3, and inhibits inflammasome formation in monocytes and microglia.

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BAL-1516

BAL-1516 Chemical Structure

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BAL-1516 Related Antibodies

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Description

BAL-1516 is an orally active NLRP3 inhibitor with human NLRP3 Kd of 14.2 nM, mouse NLRP3 Kd of 200 nM, and blood-brain barrier penetration.BAL-1516 binds to a surface groove of the NLRP3 nucleotide-binding domain, contacts FISNA and WHD subdomains, forms three hydrogen bonds to the peripheral β-strand of the triple-ATPase, and does not alter NLRP3 ATP-hydrolysis activity.BAL-1516 shows specificity for NLRP3 over other NOD-like receptors, directly binds mouse NLRP3, and inhibits inflammasome formation in monocytes and microglia[1].

IC50 & Target

NLRP3

14.2 nM (IC50)

In Vitro

BAL-1516 potently binds to the NACHT domain of human NLRP3 with a KD of 14.2 nM, and its binding site differs from that of MCC950 (HY-12815)[1].
BAL-1516 (10 μM; pre-incubated on ice for 30 min, then incubated with ATP at 25 °C for 68 min) does not inhibit the ATP hydrolysis activity of full-length human NLRP3 protein[1].
BAL-1516 binds to the wild-type mouse NLRP3NACHT domain with a Kd of 200 nM, exhibiting higher affinity than the lead compound BAL-0028 (HY-162333)[1].
BAL-1516 (incubated with Doxycycline (HY-N0565) for 4 h, followed by stimulation with Nigericin (HY-127019) for 1 h) potently inhibits Nigericin-induced NLRP3 inflammasome ASC speck formation in HEK293T cells expressing human NLRP3, with an IC50 of 14.5 nM[1].
BAL-1516 (0.256-4 μM; pre-incubated on ice for 30 min, followed by Nigericin stimulation for 30 min) potently inhibits the release of IL-1β and IL-18 from human induced pluripotent stem cell-derived microglia induced by LPS and Nigericin, with IC50 values of 11 nM and 9.0 nM, respectively[1].

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

BAL-1516 Related Antibodies

Cell Viability Assay[1]

Cell Line: Human iCell Microglial
Concentration: 0.256-4 μM
Incubation Time: 30 min pre-incubation, 30 min Nigericin stimulation (5 μg/mL, 2 h)
Result: Inhibited LPS- and Nigericin-induced IL-1β and IL-18 release from human iPSC-derived microglia, with IC50 values of 11 nM and 9.0 nM respectively, without causing significant cytotoxicity
In Vivo

BAL-1516 (100 mg/kg; p.o.; single dose) demonstrates excellent blood-brain barrier penetration and tissue stability in male CD-1 mice[1].

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

Animal Model: CD-1 mice (male)[1]
Dosage: 100 mg/kg
Administration: p.o.; single dose
Result: Reached mean plasma concentration of 1.5×104 ng/mL and mean brain concentration of 5×103 ng/g at 1 hour post-dose.
Reached mean plasma concentration of 1×103 ng/mL and mean brain concentration of 1×103 ng/g at 6 hours post-dose.
Reached mean plasma concentration of 1×102 ng/mL and mean brain concentration of 1×102 ng/g at 9 hours post-dose.
Reached mean plasma concentration of 2×102 ng/mL and mean brain concentration of 1×102 ng/g at 12 hours post-dose.
Reached mean plasma concentration of 10 ng/mL at 22 hours post-dose, with brain concentration below the limit of quantification.
Achieved a Kp coefficient (brain to plasma concentration ratio) of 0.3 at 1 hour, 0.2 at 6 hours, 0.1 at 9 hours, and 0.1 at 12 hours.
Molecular Weight

435.54

Formula

C23H25N5O2S
SMILES

CCOC1=CC(C(N([C@@H](C2=CN=C(C3=C2NN=C3)C)C)C)=O)=CC=C1C4=NC(C)=CS4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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BAL-1516 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BAL-1516BAL1516BAL 1516NOD-like Receptor (NLR)FISNANLRP3HEK293T cellsmouse NLRP3WHD subdomainsnucleotide-binding domainmonocytesmicrogliahuman NLRP3CD-1 miceInhibitorinhibitorinhibit

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