>>Signaling Pathways>> Others>>K-7174

K-7174

Catalog No.GC10983

K-7174는 새로운 세포 부착 억제제입니다. IL-1β에 의해 유도된 혈관 세포 부착 분자-1(VCAM-1)의 발현을 억제하고; 또는 TNF-α

Products are for research use only. Not for human use. We do not sell to patients.

K-7174 Chemical Structure

Cas No.: 191089-60-8

Size 가격 재고 수량
5mg
US$78.00
재고 있음
25mg
US$203.00
재고 있음
500mg
US$1,005.00
재고 있음
1g
US$1,803.00
재고 있음

Tel:(909) 407-4943 Email: sales@glpbio.com

고객 리뷰

Based on customer reviews.

  • GlpBio Citations

    GlpBio Citations
  • Bioactive Compounds Premium Provider

    Bioactive Compounds Premium Provider

Sample solution is provided at 25 µL, 10mM.

Description Chemical Properties Product Documents Related Products

Description:

IC50: 9 μM

The main function of the proteasome is to degrade unneeded or damaged proteins by proteolysis, a chemical reaction that breaks peptide bonds. Proteasome inhibition is now considered a unique and effective way to kill cancer cells that can tolerate conventional chemotherapy. K-7174 is a novel orally active proteasome inhibitor.

In vitro: Due to its proteasome inhibitary effect, K-7174 induces transcriptional repression of class I histone deacetylases (HDAC) via caspase-8-dependent degradation of Sp1, the most potent transactivator of class I HDAC genes. HDAC1 overexpression reduces the cytotoxic effect of K-7174 and abrogates histone hyperacetylation without affecting the ubiquitinated protein accumulation in K-7174-treated myeloma cells [1].

In vivo: K-7174 exhibits the therapeutic effects through its anti-proteasome activities, which is stronger when administered orally than intravenously, without obvious side effects in a murine myeloma model. In addition, K-7174 kills bortezomib-resistant myeloma cells carrying a β5-subunit mutation in vivo and primary cells from a patient resistant to bortezomib [1].

Clinical trial: Up to now, K-7174 is still in the preclinical development stage.

Reference:
[1] Kikuchi J, Yamada S, Koyama D, Wada T, Nobuyoshi M, Izumi T, Akutsu M, Kano Y, Furukawa Y.  The novel orally active proteasome inhibitor K-7174 exerts anti-myeloma activity in vitro and in vivo by down-regulating the expression of class I histone deacetylases. J Biol Chem. 2013 Aug 30;288(35):25593-602.

리뷰

Review for K-7174

Average Rating: 5 ★★★★★ (Based on Reviews and 29 reference(s) in Google Scholar.)

5 Star
100%
4 Star
0%
3 Star
0%
2 Star
0%
1 Star
0%
Review for K-7174

GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.

Required fields are marked with *

You may receive emails regarding this submission. Any emails will include the ability to opt-out of future communications.