OICR-9429
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 406821

CAS#: 1801787-56-3

Description: OICR-9429 is a potent and selective chemical probe suitable to help dissect the biological role of WDR5 (Kdisp < 100 nM). OICR-9429 selectively inhibited proliferation and induced differentiation in p30-expressing human AML cells. OICR-9429 disrupts the interaction of Wdr5 with MLL in cells, thereby selectively triggering a differentiation program in p30-expressing leukemia cells.


Price and Availability

Size
Price

10mg
USD 150
100mg
USD 850
1g
USD 3650
Size
Price

25mg
USD 250
200mg
USD 1450
2g
USD 5250
Size
Price

50mg
USD 450
500mg
USD 2150
5g
Ask price

OICR-9429, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received. Delivery time: overnight (USA/Canada); 3-5 days (worldwide). Shipping fee: from $30.00 (USA); from $45.00 (Canada); from $70.00 (international).


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 406821
Name: OICR-9429
CAS#: 1801787-56-3
Chemical Formula: C29H32F3N5O3
Exact Mass: 555.2457
Molecular Weight: 555.6022
Elemental Analysis: C, 62.69; H, 5.81; F, 10.26; N, 12.61; O, 8.64


Synonym: OICR-9429; OICR 9429; OICR9429.

IUPAC/Chemical Name: N-(4-(4-methylpiperazin-1-yl)-3'-(morpholinomethyl)-[1,1'-biphenyl]-3-yl)-6-oxo-4-(trifluoromethyl)-1,6-dihydropyridine-3-carboxamide

InChi Key: DJOVLOYCGXNVPI-UHFFFAOYSA-N

InChi Code: InChI=1S/C29H32F3N5O3/c1-35-7-9-37(10-8-35)26-6-5-22(21-4-2-3-20(15-21)19-36-11-13-40-14-12-36)16-25(26)34-28(39)23-18-33-27(38)17-24(23)29(30,31)32/h2-6,15-18H,7-14,19H2,1H3,(H,33,38)(H,34,39)

SMILES Code: O=C(C(C(C(F)(F)F)=C1)=CNC1=O)NC2=CC(C3=CC=CC(CN4CCOCC4)=C3)=CC=C2N5CCN(C)CC5


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Certificate of Analysis:

Safety Data Sheet (MSDS):

Shipping Condition:
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 Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


Additional Information

WD repeat-containing protein 5 (WDR5) is an important component of the multiprotein complex essential for activating mixed-lineage leukemia 1 (MLL1). Rearrangement of the MLL1 gene is associated with onset and progression of acute myeloid and lymphoblastic leukemias, and targeting the WDR5-MLL1 interaction may result in new cancer therapeutics. Our previous work showed that binding of small molecule ligands to WDR5 can modulate its interaction with MLL1, suppressing MLL1 methyltransferase activity.


References

1: Getlik M, Smil D, Zepeda-Velázquez C, Bolshan Y, Poda G, Wu H, Dong A,
Kuznetsova E, Marcellus R, Senisterra G, Dombrovski L, Hajian T, Kiyota T,
Schapira M, Arrowsmith CH, Brown PJ, Vedadi M, Al-Awar R. Structure-Based
Optimization of a Small Molecule Antagonist of the Interaction Between WD
Repeat-Containing Protein 5 (WDR5) and Mixed-Lineage Leukemia 1 (MLL1). J Med
Chem. 2016 Mar 24;59(6):2478-96. doi: 10.1021/acs.jmedchem.5b01630. Epub 2016 Mar
9. PubMed PMID: 26958703.

2: Grebien F, Vedadi M, Getlik M, Giambruno R, Grover A, Avellino R, Skucha A,
Vittori S, Kuznetsova E, Smil D, Barsyte-Lovejoy D, Li F, Poda G, Schapira M, Wu
H, Dong A, Senisterra G, Stukalov A, Huber KV, Schönegger A, Marcellus R, Bilban
M, Bock C, Brown PJ, Zuber J, Bennett KL, Al-Awar R, Delwel R, Nerlov C,
Arrowsmith CH, Superti-Furga G. Pharmacological targeting of the Wdr5-MLL
interaction in C/EBPα N-terminal leukemia. Nat Chem Biol. 2015 Aug;11(8):571-8.
doi: 10.1038/nchembio.1859. Epub 2015 Jul 13. Erratum in: Nat Chem Biol. 2015
Oct;11(10):815. PubMed PMID: 26167872; PubMed Central PMCID: PMC4511833.