A bridged PROTAC that drives cyclin D1 degradation
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MS28

Item No. 43040

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(4R)-N-[7-[4-[6-[(6-acetyl-8-cyclopentyl-7,8-dihydro-5-methyl-7-oxopyrido[2,3-d]pyrimidin-2-yl)amino]-3-pyridinyl]-1-piperazinyl]-1,7-dioxoheptyl]-3-methyl-L-valyl-4-hydroxy-N-[[4-(4-methyl-5-thiazolyl)phenyl]methyl]-L-prolinamide
CAS Number
2229974-73-4
Synonyms
  • XY028-133
Molecular Formula
C53H67N11O7S
Formula Weight
1002.2
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/ml
SMILES
O=C1N(C2CCCC2)C3=NC(NC4=CC=C(N5CCN(CC5)C(CCCCCC(N[C@@H](C(C)(C)C)C(N6C[C@@H](C[C@H]6C(NCC7=CC=C(C8=C(C)N=CS8)C=C7)=O)O)=O)=O)=O)C=N4)=NC=C3C(C)=C1C(C)=O
InChi Code
InChI=1S/C53H67N11O7S/c1-32-40-29-56-52(60-48(40)64(37-12-10-11-13-37)50(70)45(32)34(3)65)58-42-21-20-38(28-54-42)61-22-24-62(25-23-61)44(68)15-9-7-8-14-43(67)59-47(53(4,5)6)51(71)63-30-39(66)26-41(63)49(69)55-27-35-16-18-36(19-17-35)46-33(2)57-31-72-46/h16-21,28-29,31,37,39,41,47,66H,7-15,22-27,30H2,1-6H3,(H,55,69)(H,59,67)(H,54,56,58,60)/t39-,41+,47-/m1/s1
InChi Key
MWVNDEBEHBRZEC-WWTLGBROSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $87

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    5 mg

    $392

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    10 mg

    $653

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    Cayman Chemical
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    Product Description

    MS28 is a bridged proteolysis-targeting chimera (PROTAC) that contains palbociclib (PD 0332991; Item No. 16273) conjugated to VHL-1 (VHL ligand 1; Item No. 21591).1 It induces the degradation of cyclin D1 with a half-maximal degradation concentration (DC50) value of 950 nM in Calu-1 cells. MS28 binds to cyclin-dependent kinase 4 (Cdk4) and Cdk6 (Kds = 365 and 48 nM, respectively). It selectively induces the degradation of cyclin D1 and cyclin D3 over a panel of 57 additional kinases at 1 µM but, to a lesser extent, it does induce the degradation of Cdk4 and Cdk6 when used at a concentration of 3 µM. MS28 inhibits the growth of Calu-1 and NCI H2110 lung cancer cells (GI50s = 1 and 0.75 µM, respectively).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Xiong, Y., Zhong, Y., Yim, H., et al. Bridged proteolysis targeting chimera (PROTAC) enables degradation of undruggable targets. J. Am. Chem. Soc. 144(49), 22622-22632 (2022).