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MedKoo Cat#: 533552 | Name: UNC6852
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Description:

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

UNC6852 is a novel EED-targeted bivalent chemical degrader, selectively degrading EED, EZH2, and SUZ12 via recruitment of VHL, resulting in loss of PRC2 catalytic activity and decreased H3K27me3 levels.

Chemical Structure

UNC6852
UNC6852
CAS#2688842-08-0

Theoretical Analysis

MedKoo Cat#: 533552

Name: UNC6852

CAS#: 2688842-08-0

Chemical Formula: C43H48N10O6S

Exact Mass: 832.3479

Molecular Weight: 832.98

Elemental Analysis: C, 62.00; H, 5.81; N, 16.82; O, 11.52; S, 3.85

Price and Availability

Size Price Availability Quantity
5mg USD 110.00 Ready to ship
10mg USD 180.00 Ready to ship
25mg USD 350.00 Ready to ship
50mg USD 650.00 Ready to ship
100mg USD 1,150.00 Ready to ship
200mg USD 1,850.00 Ready to ship
500mg USD 2,950.00 Ready to ship
1g USD 3,950.00 2 weeks
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Related CAS #
No Data
Synonym
UNC6852; UNC-6852; UNC 6852
IUPAC/Chemical Name
(2S,4R)-1-((S)-2-(4-(4-(5-((Furan-2-ylmethyl)amino)-[1,2,4]triazolo[4,3-c]pyrimidin-8-yl)benzamido)butanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
InChi Key
PPNNFXIBKLCMTI-WXEAQWFJSA-N
InChi Code
InChI=1S/C43H48N10O6S/c1-26-36(60-25-48-26)29-11-9-27(10-12-29)20-45-40(57)34-19-31(54)23-52(34)41(58)37(43(2,3)4)50-35(55)8-5-17-44-39(56)30-15-13-28(14-16-30)33-22-47-42(53-24-49-51-38(33)53)46-21-32-7-6-18-59-32/h6-7,9-16,18,22,24-25,31,34,37,54H,5,8,17,19-21,23H2,1-4H3,(H,44,56)(H,45,57)(H,46,47)(H,50,55)/t31-,34+,37-/m1/s1
SMILES Code
O=C([C@H]1N(C([C@@H](NC(CCCNC(C2=CC=C(C3=CN=C(NCC4=CC=CO4)N5C3=NN=C5)C=C2)=O)=O)C(C)(C)C)=O)C[C@H](O)C1)NCC6=CC=C(C7=C(C)N=CS7)C=C6
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
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
>3 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).
HS Tariff Code
2934.99.9001
More Info
Biological target:
UNC6852 is a selective polycomb repressive complex 2 (PRC2) degrader based on PROTAC and contains an EED (embryonic ectoderm development) ligand and a von Hippel-Lindau ligand, with an IC50 of 247 nM for EED.
In vitro activity:
Degradation of PRC2 with UNC6852 blocks the histone methyltransferase activity of EZH2, decreasing H3K27me3 levels in HeLa cells and diffuse large B cell lymphoma cells containing EZH2 gain-of-function mutations. UNC6852 degrades both wild-type and mutant EZH2, and additionally displays anti-proliferative effects in this cancer model system. Reference: Cell Chem Biol. 2020 Jan 16;27(1):47-56.e15. https://pubmed.ncbi.nlm.nih.gov/31831267/
In vivo activity:
This study treated zebrafish larvae and adults with UNC6852, which proteolytically degrades polycomb repressor complex 2, and it was observed prolongation of time to occlude the caudal vein after laser injury and increased tfpia mRNA levels in larvae and adults, respectively. This study provides the basis for testing whether UNC6852 could be used as an antithrombotic drug, which could be used to study the regulation of other plasma proteins. Reference: Sci Rep. 2021 Jul 27;11(1):15238. https://pubmed.ncbi.nlm.nih.gov/34315984/
Solvent mg/mL mM
Solubility
DMSO 100.0 120.50
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 832.98 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Potjewyd F, Turner AW, Beri J, Rectenwald JM, Norris-Drouin JL, Cholensky SH, Margolis DM, Pearce KH, Herring LE, James LI. Degradation of Polycomb Repressive Complex 2 with an EED-Targeted Bivalent Chemical Degrader. Cell Chem Biol. 2020 Jan 16;27(1):47-56.e15. doi: 10.1016/j.chembiol.2019.11.006. Epub 2019 Dec 9. PMID: 31831267; PMCID: PMC7004250. 2. Raman R, Fallatah W, Al Qaryoute A, Dhinoja S, Jagadeeswaran P. Knockdown screening of chromatin binding and regulatory proteins in zebrafish identified Suz12b as a regulator of tfpia and an antithrombotic drug target. Sci Rep. 2021 Jul 27;11(1):15238. doi: 10.1038/s41598-021-94715-2. PMID: 34315984; PMCID: PMC8316476.
In vitro protocol:
1. Potjewyd F, Turner AW, Beri J, Rectenwald JM, Norris-Drouin JL, Cholensky SH, Margolis DM, Pearce KH, Herring LE, James LI. Degradation of Polycomb Repressive Complex 2 with an EED-Targeted Bivalent Chemical Degrader. Cell Chem Biol. 2020 Jan 16;27(1):47-56.e15. doi: 10.1016/j.chembiol.2019.11.006. Epub 2019 Dec 9. PMID: 31831267; PMCID: PMC7004250.
In vivo protocol:
1. Raman R, Fallatah W, Al Qaryoute A, Dhinoja S, Jagadeeswaran P. Knockdown screening of chromatin binding and regulatory proteins in zebrafish identified Suz12b as a regulator of tfpia and an antithrombotic drug target. Sci Rep. 2021 Jul 27;11(1):15238. doi: 10.1038/s41598-021-94715-2. PMID: 34315984; PMCID: PMC8316476.
1: Raman R, Fallatah W, Al Qaryoute A, Dhinoja S, Jagadeeswaran P. Knockdown screening of chromatin binding and regulatory proteins in zebrafish identified Suz12b as a regulator of tfpia and an antithrombotic drug target. Sci Rep. 2021 Jul 27;11(1):15238. doi: 10.1038/s41598-021-94715-2. PMID: 34315984; PMCID: PMC8316476. 2: Potjewyd F, Turner AW, Beri J, Rectenwald JM, Norris-Drouin JL, Cholensky SH, Margolis DM, Pearce KH, Herring LE, James LI. Degradation of Polycomb Repressive Complex 2 with an EED-Targeted Bivalent Chemical Degrader. Cell Chem Biol. 2020 Jan 16;27(1):47-56.e15. doi: 10.1016/j.chembiol.2019.11.006. Epub 2019 Dec 9. PMID: 31831267; PMCID: PMC7004250.