BMS-986397 free base · Synonyms: CC-91633

BMS-986397 is a first-in-class molecular glue degrader of Casein Kinase 1α (CK1α).

For research use only. Not for human or veterinary use.

Target Molecular Glues Ligands for E3 Ligase Casein Kinase Apoptosis MDM-2/p53

Research area Inflammation/Immunology Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

BMS-986397 structure

CAS No.: 2564486-44-6

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
500 mg	USD 745.00	BP-00104-500mg	In stock	Get quote
1 g	USD 1,181.00	BP-00104-1g	In stock	Get quote
2 g	USD 2,225.00	BP-00104-2g	In stock	Get quote
3 g	USD 3,160.00	BP-00104-3g	In stock	Get quote
5 g	Inquire	BP-00104-5g	In stock	Inquire
10 g	Inquire	BP-00104-10g	In stock	Inquire

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Description

BMS-986397 is a first-in-class molecular glue degrader of Casein Kinase 1α (CK1α).

Biological activity

In Vitro BMS‑986397 demonstrates significant anti‑proliferative activity in TP53 wild‑type AML cell lines via potent and selective degradation of CK1α. Degradation of CK1α leads to stabilization of p53 protein and upregulation of its downstream transcriptional targets, including p21, PUMA and BAX, thereby inducing cell cycle arrest and acute apoptosis in AML cells.

Identifiers

SMILES: O=C1CC[C@@H](C(N1)=O)N2CC3=C(C2=O)C=CC(C(N[C@@H](C(F)(F)F)C4=NC=CC=C4Cl)=O)=C3
InChIKey: DGAWFEDONPXNNP-WMLDXEAASA-N

Specifications

MW (average): 480.8240
Formula: C₂₁H₁₆ClF₃N₄O₄
CAS No.: 2564486-44-6
Physical state: Solid
Color: White to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder 4℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

In vitro: DMSO : 100 mg/mL

Documents

References

[1]. Fuchs O. Targeting cereblon in hematologic malignancies. Blood Rev. 2023 Jan;57:100994. doi: 10.1016/j.blre.2022.100994. Epub 2022 Jul 31. PMID: 35933246.

[2]. Jimenez C, et al. Blood, 2024, 144: 1395.

[3]. https://acs.digitellinc.com/p/s/discovery-of-bms-986397-a-first-in-class-molecular-glue-degrader-of-casein-kinase-1a-ck1a-for-the-treatment-of-acute-myeloid-leukemia-aml-harboring-functional-tp53-605249

Same target

Search Molecular Glues

Same research area

Search Inflammation/Immunology