1. Epigenetics
  2. Histone Methyltransferase
  3. MS1943

MS1943 

Cat. No.: HY-133129
Handling Instructions

MS1943 is a first-in-class, orally bioavailable EZH2 selective degrader, with an IC50 of 120 nM. MS1943 significantly reduces EZH2 protein levels in numerous triple-negative breast cancer (TNBC) and other cancer and noncancerous cell lines. MS1943 effectively blocks proliferation of multiple TNBC and other cancer cell lines.

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

MS1943 Chemical Structure

MS1943 Chemical Structure

CAS No. : 2225938-17-8

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Description

MS1943 is a first-in-class, orally bioavailable EZH2 selective degrader, with an IC50 of 120 nM. MS1943 significantly reduces EZH2 protein levels in numerous triple-negative breast cancer (TNBC) and other cancer and noncancerous cell lines. MS1943 effectively blocks proliferation of multiple TNBC and other cancer cell lines[1].

IC50 & Target

EZH2

120 nM (IC50)

In Vitro

MS1943 (0.625-5 μM; 3 days)inhibits cell growth with an GI50 of 2.2 µM[1].
MS1943 (0.625-5 μM; 4 days)induces cell death in MDA-MB-468 cells. MS1943 effectively reduces EZH2 levels in BT549, HCC70 and MDA-MB-231 TNBC cells, as well as KARPAS-422 and SUDHL8 lymphoma cells and PNT2 non-cancerous prostate cells[1].
MS1943 (1.25-5.0μM; 2 days) inhibits EZH2 and SUZ12 protein levels in a concentration- and timedependent manner, without affecting EED protein levels, whereas the H3K27me3 mark was also suppressed[1].

Cell Viability Assay[1]

Cell Line: MDA-MB-468 cells
Concentration: 0.625, 1.25, 2.5, 5 μM
Incubation Time: 3 days
Result: Inhibits cell growth with an GI50 of 2.2 µM.

Western Blot Analysis[1]

Cell Line: MDA-MB-468 cells
Concentration: 1.25, 2.5, 5.0 μM
Incubation Time: 2 days
Result: Reduced EZH2 protein levels in a concentration- and time-dependent manner.
In Vivo

MS1943 (150 mg/kg body weight; i.p.; once daily for 36 days) suppresses tumor growth[1].
MS1943 induces apoptosis in the MDA-MB-468 xenograft model[1].
A single i.p. injection of MS1943 at 50 mg/kg body weight achieved a peak plasma concentration (Cmax) of 2.9 µM and resulted in plasma concentrations above its cellular IC50 value for ~2h. A single 150 mg/kg body weight p.o. dose achieved Cmax of 1.1 µM, but plasma concentrations were below the cellular IC50 value[1].

Animal Model: Eight-week-old female BALB/c nude mice (MDA-MB-468 xenografts)[1]
Dosage: 150 mg/kg body weight
Administration: i.p.; once daily for 36 days
Result: Suppresses tumor growth.
Molecular Weight

718.93

Formula

C₄₂H₅₄N₈O₃

CAS No.

2225938-17-8

SMILES

CC(C)N(N=C1)C2=C1C(C(NCC3=C(C)C=C(C)NC3=O)=O)=CC(C4=CC=C(N=C4)N(CC5)CCN5CCNC(CC67C[[email protected]]8C[[email protected]](C[[email protected]](C8)C7)C6)=O)=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
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Keywords:

MS1943MS 1943MS-1943Histone Methyltransferasetriple-negativebreastcancerTNBCproliferationfirst-in-classcytotoxicdegradermethyltransferaseapoptosisInhibitorinhibitorinhibit

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MS1943
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