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Cat. No.: HY-144283

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BLK-IN-1

BLK-IN-1 (compound 1) is a selective and covalent inhibitor of B-Lymphoid tyrosine kinase (BLK) and BTK, with IC₅₀s of 18.8 nM and 20.5 nM, respectively. BLK-IN-1 can be used for the research of cancer.

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

CAS No.: 1431727-00-2
Formula: C₂₉H₂₃F₃N₆O₃
Molecular Weight:560.53

Storage:

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

Data Sheet (263 KB)

BLK-IN-1 Chemical Structure

CAS No.: 1431727-00-2

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Use of MCE Products

Fluorescent Dye

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

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

Biological Activity

Description

IC₅₀ & Target

IC50: 18.8 nM (BLK), 20.5 nM (BTK)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
DOHH-2	GI₅₀	0.073 μM Compound: 31	Cytotoxicity against human DOHH2 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo luminescent cell viability assay Cytotoxicity against human DOHH2 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo luminescent cell viability assay	[PMID: 24915291]
Pfeiffer	GI₅₀	0.008 μM Compound: 31	Cytotoxicity against human Pfeiffer cells assessed as growth inhibition after 72 hrs by CellTiter-Glo luminescent cell viability assay Cytotoxicity against human Pfeiffer cells assessed as growth inhibition after 72 hrs by CellTiter-Glo luminescent cell viability assay	[PMID: 24915291]
Ramos	IC₅₀	14 nM Compound: 31	Inhibition of Btk phosphorylation at Tyr551 in human Ramos cells after 1 hr by Western blot analysis Inhibition of Btk phosphorylation at Tyr551 in human Ramos cells after 1 hr by Western blot analysis	[PMID: 24915291]
Ramos	IC₅₀	8.5 nM Compound: 31	Inhibition of Btk in human Ramos cells assessed as inhibition of PLC-gamma2 phosphorylation at Tyr1217 after 1 hr by Western blot analysis Inhibition of Btk in human Ramos cells assessed as inhibition of PLC-gamma2 phosphorylation at Tyr1217 after 1 hr by Western blot analysis	[PMID: 24915291]
SU-DHL-6	GI₅₀	0.038 μM Compound: 31	Cytotoxicity against human SU-DHL6 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo luminescent cell viability assay Cytotoxicity against human SU-DHL6 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo luminescent cell viability assay	[PMID: 24915291]
WSU-NHL	GI₅₀	0.031 μM Compound: 31	Cytotoxicity against human WSU-NHL cells assessed as growth inhibition after 72 hrs by CellTiter-Glo luminescent cell viability assay Cytotoxicity against human WSU-NHL cells assessed as growth inhibition after 72 hrs by CellTiter-Glo luminescent cell viability assay	[PMID: 24915291]

Chemical Information

CAS No. 1431727-00-2
Molecular Weight 560.53
Formula C₂₉H₂₃F₃N₆O₃
SMILES

O=C(NC1=CN=C(NC2=CC=CC(NC(C=C)=O)=C2)N=C1)C3=CC(NC(C4=CC=CC(C(F)(F)F)=C4)=O)=CC=C3C
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 (263 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]. Fu T, et, al. Discovery of selective irreversible inhibitors of B-Lymphoid tyrosine kinase (BLK). Eur J Med Chem. 2022 Feb 5;229:114051. [Content Brief]

Calculators

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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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