2. PROTAC Protein Tyrosine Kinase/RTK MAPK/ERK Pathway Stem Cell/Wnt
  3. PROTACs Btk Syk MEK ERK
  4. UBX-382

UBX-382 is an orally active BTK PROTAC degrader with a DC50 of 4.56 nM. UBX-382 inhibits B-cell receptor signaling by targeting BTK. UBX-382 shows superior degradation activity for wild-type and mutant BTK proteins. UBX-382 inhibits tumor growth in murine xenograft models harboring wild-type or C481S mutant BTK-expressing TMD-8 cells. UBX-382 can be used for the study of B-cell-related blood cancers.

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UBX-382

UBX-382 Chemical Structure

CAS No. : 2884554-45-2

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Based on 1 publication(s) in Google Scholar

UBX-382 Related Antibodies

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Description

UBX-382 is an orally active BTK PROTAC degrader with a DC50 of 4.56 nM. UBX-382 inhibits B-cell receptor signaling by targeting BTK. UBX-382 shows superior degradation activity for wild-type and mutant BTK proteins. UBX-382 inhibits tumor growth in murine xenograft models harboring wild-type or C481S mutant BTK-expressing TMD-8 cells. UBX-382 can be used for the study of B-cell-related blood cancers[1].

IC50 & Target[1]

Cereblon

 

In Vitro

UBX-382 (0.00001-10 nM, 0.5-48 h) induces potent BTK degradation with a DC 50 of 4.56 nM in TMD-8 cells[1].
UBX-382 (0.0001-10 μM, 3-5 days) inhibits the proliferation of TMD8 (IC50 = 14 nM), WSU-DLCL2 (IC50 = 18 nM), OCI-Ly3 (IC50 = 199 nM) and U2932 (IC50 = 21 nM) measured by the Cell Titer-Glo assay in duplicates[1].
UBX-382 (10 nM, 24 h) significantly inhibits CCL3 and CCL4 secretion induced by BCR signal activation in TMD-8 cells[1].
UBX-382 (100 nM, 6-24 h) inhibits the phosphorylation of BTK Y223, SYK, MEK, and ERK in U2932 cells[1].
UBX-382 (0.1-10 μM, 24 h) effectively degrades wild-type and various BTK mutants (E41K, C481S/R/T/Y/F, L528W) in HEK293 cells and strongly suppresses their phosphorylation[1].

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

UBX-382 Related Antibodies

Western Blot Analysis[1]

Cell Line: U2932 cells
Concentration: 100 nM
Incubation Time: 6, 24 h
Result: Showed far more effective inhibition of BTK Y223 phosphorylation than Ibrutinib (HY-10997), Acalabrutinib (HY-17600), and Nemtabrutinib (ARQ-531) (HY-112215) in U2932 cells.
Inhibited the phosphorylation of SYK, MEK, and ERK.
In Vivo

UBX-382 (3-30 mg/kg, p.o., once daily, 21 days) inhibits the growth of tumor in TMD-8 xenograft models and TMD-8 BTK C481S xenograft model[1].

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

Animal Model: TMD-8 cells (1 × 107 in Matrigel) were subcutaneously injected into the flanks of 6-week-old CB17/severe combined immunodeficient mice[1]
Dosage: 3, 10, 30 mg/kg
Administration: p.o. once daily for 21 days
Result: Achieved complete tumor regression in TMD-8 xenograft models.
Showed no significant changes in body weight and no other clinical toxicity signs during the experiment.
Reduced BTK levels in tumors of TMD-8 xenograft models.
Animal Model: TMD-8 BTK C481S cells were subcutaneously inoculated into the right flank of male CB17/severe combined immunodeficient mice[1]
Dosage: 3, 10, 30 mg/kg
Administration: p.o. once daily for 21 days
Result: Induced remarkable dose-dependent tumor regression in TMD-8 BTK C481S xenograft models, while Ibrutinib failed to inhibit tumor growth.
Molecular Weight

752.86

Formula

C42H44N10O4
CAS No.
Appearance

Solid

Color

Light yellow to green yellow

SMILES

O=C1C2=CC=C(N3CCC(CC3)CN4CC5=CC(NC6=NC7=C(C(NC8=C(C)C=CC=C8C)=NN7C)C=N6)=CC=C5CC4)C=C2C(N1C9C(NC(CC9)=O)=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation
References
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UBX-382 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:

UBX-3822884554-45-2UBX382UBX 382PROTACsBtkSykMEKERKBruton tyrosine kinaseSpleen tyrosine kinaseMitogen-activated protein kinase kinaseMAPKKMAP2KExtracellular signal regulated kinasesB-cell lymphomasTMD-8in murine xenograft models of TMD-8 cellsB-cell receptorBTKSYKERK,Inhibitorinhibitorinhibit

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