1. PROTAC Epigenetics Stem Cell/Wnt Protein Tyrosine Kinase/RTK JAK/STAT Signaling
  2. PROTACs JAK
  3. SJ1008030

SJ1008030 (compound 8) is a JAK2 PROTAC which selectively degrades JAK2. SJ1008030 inhibits MHH–CALL-4 cell growth with an IC50 of 5.4 nM. SJ1008030 can be used for the research of leukemia.
(Pink: JAK2 ligand (HY-15315); Blue: Cereblon ligand (HY-W834174); Black: linker).

For research use only. We do not sell to patients.

SJ1008030

SJ1008030 Chemical Structure

CAS No. : 2863634-96-0

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Description

SJ1008030 (compound 8) is a JAK2 PROTAC which selectively degrades JAK2. SJ1008030 inhibits MHH–CALL-4 cell growth with an IC50 of 5.4 nM. SJ1008030 can be used for the research of leukemia[1]. (Pink: JAK2 ligand (HY-15315); Blue: Cereblon ligand (HY-W834174); Black: linker).

IC50 & Target

IC50: 32.09 nM (MHH-CALL-4), 33.41 nM (MHH-CALL4-GSPT1-WT), 33.55 nM (MHH-CALL-4-GSPT1-G575N) [1]

In Vitro

SJ1008030 (compound 8) (72 h) shows activity in CRLF2r cell lines (MHH–CALL-4), with an IC50 of 5.4 nM[1].
SJ1008030 (0-4.3 μM; 72 h) degrades JAKs, GSPT1, and IKZF1 in a dose-dependent manner in MHH–CALL-4 cells[1].
SJ1008030 (0-10 μM; 24h) dose-dependently degrades JAK2 and GSPT1 protein in xenograft bone marrow SJBALL021415 cells, indicating the inhibition of JAK-STAT signaling pathway[1].

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

Cell Cytotoxicity Assay[1]

Cell Line: The CRLF2r cell lines MHH–CALL-4, KOPN49, MHH–CALL-2, KOP N75, NALM-6 and 697
Concentration: 0-3 μM
Incubation Time: 72 hours
Result: Showed best activity in MHH–CALL-4 cells with an EC50 value of 5.4 nM.

Western Blot Analysis[1]

Cell Line: MHH–CALL-4 cells
Concentration: 1 nM, 10 nM, 100 nM, 1 μM and 4.3 μM
Incubation Time: 72 hours
Result: Significantly degradated JAK2 in MHH–CALL-4 cells dose-dependently while showed weakly effect to JAK1, JAK3 and GSPT1.

Western Blot Analysis[1]

Cell Line: Xenograft SJBALL021415 bone marrow cells
Concentration: 1, 10, 100, 1000 and 1000 nM
Incubation Time: 24 hours
Result: Near-completely degradated JAK2 in a dose-dependent way while showed no effect on GSPT1.
Molecular Weight

873.94

Formula

C42H43N13O7S

CAS No.
SMILES

O=S(CC)(N1CC(N2C=C(C=N2)C3=C4C=CNC4=NC(NC5=CC=C(C=C5)C(NCCN6CCN(CC6)C7=CC=C8C(N(C9CCC(NC9=O)=O)C(C8=C7)=O)=O)=O)=N3)(CC#N)C1)=O

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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  • 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:
SJ1008030
Cat. No.:
HY-147330
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