SML1465
UNC0379 trifluoroacetate salt
≥98% (HPLC)
동의어(들):
6,7-Dimethoxy-2-(pyrrolidin-1-yl)-N-(5-(pyrrolidin-1-yl)-pentyl)quinazolin-4-amine trifluoroacetate salt
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모든 사진(1)
About This Item
실험식(Hill 표기법):
C23H35N5O2 · xC2HF3O2
CAS Number:
Molecular Weight:
413.56 (free base basis)
MDL number:
UNSPSC 코드:
12352200
PubChem Substance ID:
NACRES:
NA.77
추천 제품
Quality Level
분석
≥98% (HPLC)
형태
powder
저장 조건
desiccated
색상
white to beige
solubility
H2O: 5 mg/mL, clear
저장 온도
2-8°C
SMILES string
COC1=C(OC)C=C(N=C(N2CCCC2)N=C3NCCCCCN4CCCC4)C3=C1
InChI
1S/C23H35N5O2/c1-29-20-16-18-19(17-21(20)30-2)25-23(28-14-8-9-15-28)26-22(18)24-10-4-3-5-11-27-12-6-7-13-27/h16-17H,3-15H2,1-2H3,(H,24,25,26)
InChI key
WEXCGGWTIDNVNT-UHFFFAOYSA-N
생화학적/생리학적 작용
SETD8 expression is observed in cancers such as bladder cancer, chronic myelogenous leukemia, hepatocellular carcinoma, non‐small‐cell lung carcinoma, prostate cancer, small‐cell lung carcinoma. Therefore inhibition of SETD8 (SET‐domain containing protein) by UNC0379 might prevent the progression of cancer.
UNC0379 is the first substrate-competitive inhibitor of the lysine methyltransferase SETD8, the only known methyltransferase that catalyzes monomethylation of histone H4 lysine 20 (H4K20). HK420 methylation has been implicated in the regulation of a variety of biological processes including the DNA damage response. UNC0379 is selective for SETD8 over 15 other methyltransferases, with an IC50 value of 7.3 μM for SETD8 compared to IC50 vlaues over 100 μM for other methyltransferases.
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point (°F)
Not applicable
Flash Point (°C)
Not applicable
시험 성적서(COA)
제품의 로트/배치 번호를 입력하여 시험 성적서(COA)을 검색하십시오. 로트 및 배치 번호는 제품 라벨에 있는 ‘로트’ 또는 ‘배치’라는 용어 뒤에서 찾을 수 있습니다.
Olivia G Dobbs et al.
BMC biology, 21(1), 175-175 (2023-08-15)
Cip1-interacting zinc finger protein 1 (CIZ1) forms RNA-dependent protein assemblies that stabilise epigenetic state, notable at the inactive X chromosome in females. CIZ1 has been linked with a range of human cancers and in mice genetic deletion of CIZ1 manifests
Dysregulation of protein methyltransferases in human cancer: an emerging target class for anticancer therapy.
Hamamoto R and Nakamura Y
Cancer Science, 107(4), 377-384 (2016)
Miku Wada et al.
Biomolecules, 10(12) (2020-12-20)
The histone methyltransferase SETD8, which methylates the lysine 20 of histone H4 (H4K20), is reportedly involved in human carcinogenesis along with nonhistone proteins such as p53. However, its expression profiles and functions in the context of high-grade serous ovarian carcinoma
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