An inhibitor of the SF3B complex
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H3B-8800

Item No. 42106

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-methyl-1-piperazinecarboxylic acid, (2S,3S,4E,6S,7R,10R)-7,10-dihydroxy-3,7-dimethyl-2-[(1E,3E,5R)-1-methyl-5-(2-pyridinyl)-1,3-hexadien-1-yl]-12-oxooxacyclododec-4-en-6-yl ester
CAS Number
1825302-42-8
Molecular Formula
C31H45N3O6
Formula Weight
555.7
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Slightly soluble: 0.1-1 mg/mlEthanol: Slightly soluble: 0.1-1 mg/ml
SMILES
O=C(N1CCN(CC1)C)O[C@H]2/C=C/[C@@H]([C@H](OC(C[C@@H](CC[C@]2(O)C)O)=O)/C(C)=C/C=C/[C@H](C3=CC=CC=N3)C)C
InChi Code
InChI=1S/C31H45N3O6/c1-22(26-11-6-7-16-32-26)9-8-10-23(2)29-24(3)12-13-27(39-30(37)34-19-17-33(5)18-20-34)31(4,38)15-14-25(35)21-28(36)40-29/h6-13,16,22,24-25,27,29,35,38H,14-15,17-21H2,1-5H3/b9-8+,13-12+,23-10+/t22-,24+,25-,27+,29-,31-/m1/s1
InChi Key
YOIQWBAHJZGRFW-WVRLKXNASA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $131

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    1 mg

    $249

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    5 mg

    $655

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    10 mg

    $1,048

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    Cayman Chemical
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    Product Description

    H3B-8800 is an inhibitor of the splicing factor 3B (SF3B) complex.1 It binds to SF3B complexes containing wild-type SF3B (IC50 = 1.4 nM) or various SF3B mutations (IC50s = 0.3-1.8 nM) in cell-free assays. It inhibits splicing of canonical and aberrant pre-mRNA junctions induced by SF3B subunit 1 (SF3B1) in HEK293T nuclear extracts overexpressing SF3B1 with a lysine-to-glutamate mutation at residue 700 (SF3B1K700E). H3B-8800 selectively inhibits the growth of, and induces apoptosis in, Panc 05.04 pancreatic cancer cells expressing mutant SF3B over Panc 10.05, HAPF-II, and CFPAC-1 pancreatic cancer cells expressing wild-type SF3B in a concentration-dependent manner. It reduces tumor growth in a K562 chronic myeloid leukemia (CML) mouse xenograft model using K562 cells expressing wild-type SF3B1 when administered at a dose of 8 mg/kg or K562 cells expressing SF3B1K700E when administered at doses of 2, 4, or 8 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Seiler, M., Yoshimi, A., Darman, R., et al. H3B-8800, an orally available small-molecule splicing modulator, induces lethality in spliceosome-mutant cancers. Nat. Med. 24(4), 497-504 (2018).