175205-09-1

175205-09-1 structure

Name: Activator 42
Chemical Name: 5-[3,5-Bis(trifluoromethyl)phenyl]tetrazole
CAS Number: 175205-09-1
Molecular Formula: C₉H₄F₆N₄
Molecular Weight: 282.14500
Catalog: Signaling Pathways Metabolic Enzyme/Protease HIF/HIF Prolyl-Hydroxylase
Create Date: 2019-01-21 16:31:30
Modify Date: 2024-01-03 10:04:12
KG-548 is an ARNT/TACC3 disruptor and a HIF-1α inhibitor. KG-548 directly interferes with ARNT/TACC3 complex formation by competing with TACC3 for binding to the ARNT PAS-B domain. ARNT is the aryl hydrocarbon receptor nuclear translocator, also known as HIF-β[1][2].

Name	5-[3,5-Bis(trifluoromethyl)phenyl]tetrazole
Synonyms	MFCD00052524 5-[3,5-bis(trifluoromethyl)phenyl]-2H-tetrazole

Description	KG-548 is an ARNT/TACC3 disruptor and a HIF-1α inhibitor. KG-548 directly interferes with ARNT/TACC3 complex formation by competing with TACC3 for binding to the ARNT PAS-B domain. ARNT is the aryl hydrocarbon receptor nuclear translocator, also known as HIF-β[1][2].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Metabolic Enzyme/Protease >> HIF/HIF Prolyl-Hydroxylase
Target	HIF-β[1]; HIF-1α[2]
In Vitro	HIF is a heterodimer of two bHLH-PAS (basic Helix Loop Helix-Per-ARNT-Sim) subunits, including a HIF-α paralog (HIF-1α, -2α, -3α) and aryl hydrocarbon receptor nuclear translocator (ARNT, also known as HIF-β)[1]. KG-548 (0-250 μM; 16 h for over night) exhibits the great reduction of ARNT/CCC complex formation for both coactivators, and also disrupts ARNT2 PAS-B/TACC3 interactions[1]. KG-548 (0-2 mM; 16 h for over night) dose-dependently breaks up the (320 μM) ARNT PAS-B/TACC3 complex in vitro and in cell lysate with an IC50 value of 25 μM[1]. KG-548 significantly inhibits lactate production of glycolysis on in FaDu hypopharyngeal carcinoma cells[2]. Western Blot Analysis[1] Cell Line: HEK293T cell lysates Concentration: 0, 5, 50, 100, 250, 500 μM and 1 mM, 2 mM Incubation Time: 16 hours Result: Weakened the ARNT/TACC3 interaction from 5 μM to 500 μM dose-dependently, and decreased the protein intense of ARNT associated with immunoprecipitated TACC3 protein by 82% (500 μM), 59% (1 mM), 43% (2 mM), respectively.

Symbol	GHS02, GHS07
Signal Word	Danger
Hazard Statements	H225-H302 + H332-H315-H319
Precautionary Statements	P210-P305 + P351 + P338
Personal Protective Equipment	Eyeshields;Faceshields;full-face respirator (US);Gloves;multi-purpose combination respirator cartridge (US);type ABEK (EN14387) respirator filter
Hazard Codes	Xi
Risk Phrases	25-36/37/38
Safety Phrases	26-45
RIDADR	UN 1648 3 / PGII
HS Code	2933990090
Flash Point(F)	41 °F
Flash Point(C)	5 °C

27126-93-8

~60%

175205-09-1

Literature: Sigma-Aldrich Co. Patent: US2006/247431 A1, 2006 ;

Precursor 1
27126-93-8
DownStream 0

HS Code	2933990090
Summary	2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%