1. PROTAC Stem Cell/Wnt JAK/STAT Signaling
  2. STAT PROTACs
  3. XD2-149

XD2-149 is a PROTAC targeting STAT3. XD2-149 consists of PROTAC target protein ligand Napabucasin (HY-13919) (red part), E3 ligase Thalidomide (HY-14658) (black part), and linker NH2-C5-Azacyclohexane-N-Boc (HY-159572) (blue part). The E3 ligase + linker conjugate is Thalidomide-NH-C5-azacyclohexane-N-Boc (HY-159571), and the active control of the target protein ligand is Thalidomide acid (HY-159573)[1].

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XD2-149

XD2-149 Chemical Structure

CAS No. : 2710221-08-0

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Description

XD2-149 is a PROTAC targeting STAT3. XD2-149 consists of PROTAC target protein ligand Napabucasin (HY-13919) (red part), E3 ligase Thalidomide (HY-14658) (black part), and linker NH2-C5-Azacyclohexane-N-Boc (HY-159572) (blue part). The E3 ligase + linker conjugate is Thalidomide-NH-C5-azacyclohexane-N-Boc (HY-159571), and the active control of the target protein ligand is Thalidomide acid (HY-159573)[1].

IC50 & Target

STAT3[1]

Cellular Effect
Cell Line Type Value Description References
BXPC-3 IC50
0.8 μM
Compound: 3-6d; XD2-149
Antiproliferative activity against human BxPC-3 cells assessed as reduction in cell viability incubated for 3 days by MTT assay
Antiproliferative activity against human BxPC-3 cells assessed as reduction in cell viability incubated for 3 days by MTT assay
[PMID: 33506674]
BXPC-3 IC50
1.2 μM
Compound: 3-6d; XD2-149
Antiproliferative activity against human BxPC-3 cells harboring ZFP91siRNA assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human BxPC-3 cells harboring ZFP91siRNA assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 33506674]
BXPC-3 IC50
2.1 μM
Compound: 3-6d; XD2-149
Antiproliferative activity against ZFP91 knockdown human BxPC-3 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against ZFP91 knockdown human BxPC-3 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 33506674]
HEK293 IC50
8.7 μM
Compound: 3-6d; XD2-149
Antiproliferative activity against human HEK293 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
Antiproliferative activity against human HEK293 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
[PMID: 33506674]
MIA PaCa-2 IC50
1 μM
Compound: 3-6d; XD2-149
Antiproliferative activity against human MIA PaCa-2 cells assessed as reduction in cell viability incubated for 3 days by MTT assay
Antiproliferative activity against human MIA PaCa-2 cells assessed as reduction in cell viability incubated for 3 days by MTT assay
[PMID: 33506674]
Molecular Weight

693.74

Formula

C38H39N5O8

CAS No.
SMILES

O=C(C1=CC2=C(C(C3=C(C2=O)C=CC=C3)=O)O1)NCCN4CCC(CCCCCNC5=CC=CC(C(N6C7C(NC(CC7)=O)=O)=O)=C5C6=O)CC4

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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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.

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Product Name:
XD2-149
Cat. No.:
HY-159570
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