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Cat. No.: HY-147330

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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.

CAS No.: 2863634-96-0
Formula: C₄₂H₄₃N₁₃O₇S
Molecular Weight:873.94

Storage:

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

Data Sheet (272 KB)

SJ1008030 Chemical Structure

CAS No.: 2863634-96-0

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

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]

All PROTACs Isoforms :

All JAK Isoforms :

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.

Chemical Information

CAS No. 2863634-96-0
Molecular Weight 873.94
Formula C₄₂H₄₃N₁₃O₇S
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
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Chang Y, et al. Degradation of Janus kinases in CRLF2-rearranged acute lymphoblastic leukemia. Blood. 2021 Dec 9;138(23):2313-2326. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References

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SJ1008030

All PROTACs Isoforms

All JAK Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

SJ1008030 Related Classifications

HY-147330 Related Classifications