Epigenetic Writers Inhibitor & Activator

Epigenetic Writers란?

Epigenetic writer는 후성유전적 표지를 붙여줍니다. 크게 5종류가 있는데, 1) 히스톤에 methyl기 transfer를 촉매해주는 histone methyltransferase, 2) acetyl기를 transfer해주는 histone acetyltransferase, 3) histone tail을 phosphorylation 해주는 JAK2, histone 단백질을 phosphrylation해주는 Haspin, Pim-1, PKC, ATM/ATR kinase, 4) 히스톤 단백질을 ubiquitination해주는 E2ubiquitin conjugase, E3 ubiquitin ligase, 그리고 5) DNA에 methyl기를 붙여주는 DNA methyltransferase 등이 있습니다.

Histone Methyltransferases

Histone methyltransferase는, 표적 아미노산기에 따라 lysine methyltransferase와 arginine methyltransferase로 구분합니다.

Lysine methyltransferase는 PKMT라고도 알려져 있으며, 보조인자 S로부터 메틸기의 전달을 촉매합니다.

Arginine methyltransferase는 PRMT라고도 알려져 있으며, 단일메틸화 또는 이중 메틸화를 생성할 수 있고, 이중메틸화는 대칭적 또는 비대칭적으로 할 수 있습니다. 대칭적 이중메틸화는 유전자 억제에 관여하고, 비대칭적 이중메틸화는 유전자 활성에 관여합니다.

	Cat. No.	Product	Activity
Protein Arginine Methyl transferase Inhibitors	5128	C 21	Selective PRMT1 inhibitor
	6516	EPZ 015666	Potent and selective PRMT5 inhibitor
	5202	Furamidine dihydrochloride	Selective PRMT1 inhibitor
	5777	GSK 591 dihydrochloride	Potent and selective PRMT5 inhibitor
	5713	MS 023 dihydrochloride	Potent and selective type I PRMT inhibitor
	6825	SGC 3027	Potent and selective PRMT7 inhibitor
	7182	SGC 6870	Potent and selective PRMT6 allosteric inhibitor
	5367	SGC 707	Potent and selective allosteric inhibitor of PRMT3
	5099	TC-E 5003	Selective PRMT1 inhibitor
	6008	TP 064	Potent and selective PRMT 4 inhibitor
	5057	UNC 2327	Allosteric inhibitor of PRMT3
Controls	6838	SGC 3027N	Negative control for SGC 3027 (Cat. No. 6825)
	7184	SGC 6870N	Negative control for SGC 6870 (Cat. No. 7182)
	5450	XY1	Negative control of SGC 707 (Cat. No. 5367)

Histone Acetyltransferase

Histone Acetyltransferase(HAT)는 lysine acetyltransferase(KAT)라고도 알려져 있으며, acetyl-CoA에서 lysine기에 acetyl기를 옮기는 acetylation을 촉매합니다. 반대 작용은 histone deacetylases(HDACs)에 의해 이루어집니다.

히스톤 꼬리의 lysine기에 Acetyl Co-A로부터 acetyl기를 옮기면 히스톤 꼬리의 양전하를 중화시켜 DNA에 대한 친화력을 약화시켜 크로마틴 응축을 감소시킵니다. 전사인자와 중합효소를 recruitment를 가능하게 하여 유전자 발현을 촉진시킵니다.

	Cat. No.	Product	Activity
Histone Acetyltransferase Inhibitors	6387	A 485	Potent and selective p300/CBP inhibitor; orally bioavailable
	3084	Anacardic acid	Noncompetitive PCAF/p300 inhibitor
	4200	C 646	Selective p300/CBP inhibitor
	5646	EML 425	Reversible and non-competitive CBP/p300 inhibitor
	7270	iP300w	Potent p300/CBP inhibitor
	5045	L002	p300 inhibitor
	5103	Lys-CoA	Selective p300 inhibitor
	4903	NU 9056	Inhibitor of KAT5 (Tip60)
	5964	SI-2 hydrochloride	Steroid receptor coactivator 3 (SRC-3) inhibitor
	6692	WM 1119	High affinity KAT6A (MOZ) competitive inhibitor
	7366	WM 3835	Lysine acetyltransferase HBO1 (KAT7) inhibitor
	6693	WM 8014	Potent and selective KAT6A and KAT6B inhibitor
Others	4891	I-CBP 112	Selective CBP/p300 BRD inhibitor
Others	4889	SGC-CBP30	Potent CBP/p300 BRD inhibitor

Phosphorylation

Junus Kinase(JAK)은 tyrosine kinase family로 cytokine receptor와 연관된다. JAK에 의해 히스톤 H3(H3Y41)이 phosphorylation 되면, HP1α와 크로마틴의 결합을 방해하여 DNA의 접근성을 높여주어 oncogene Imo2의 전사를 활성화해준다.

그 외, Haspin, Pim-1, PKC, ATM/ATR kinase 등도 히스톤의 phosphorylation을 하여 유전자 발현을 조절한다.

	Cat. No.	Product	Activity
JAK Inhibitors	414	AG 490	JAK2, JAK3 inhibitor. Also EGFR-kinase inhibitor
	4580	Atiprimod dihydrochloride	JAK2 inhibitor
	5617	AZD 1480	Potent and selective JAK2 inhibitor; antiangiogenic
	7222	Baricitinib	Highly potent JAK1 and JAK2 inhibitor; also inhibits JAK3 and Tyk2
	4500	Cercosporamide	Potent Mnk2 inhibitor; also inhibits JAK3
	4556	CP 690550 citrate	Potent JAK inhibitor
	1571	Cucurbitacin I	Selective inhibitor of STAT3/JAK2 signaling
	3395	Lestaurtinib	JAK2, FLT3 and TrkA inhibitor; also inhibits AurA and AurB
	5818	NVP BSK 805	Potent JAK2 inhibitor; orally bioavailable
	6506	PF 06551600 malonate	Potent and selective JAK3 inhibitor
	6577	Pyridone 6	Potent pan-JAK inhibitor; induces intermediate mesoderm; cell-permeable
	7064	Ruxolitinib	Potent and selective JAK1/JAK2 inhibitor; orally bioavailable
	7048	Ruxolitinib phosphate	Phosphate salt of Ruxolitinib (Cat. No. 7064); potent and selective JAK1/JAK2 inhibitor
	3035	SD 1008	JAK2/STAT3 signaling pathway inhibitor

Ubiquitination

히스톤 단백질 H2A와 H2B는 E2 ubiquitin conjugases와 E3 ubiquitinligase가 함께 monoubiquitination 하게 한다. Ubiquitin E3 Ligase (EC 6.3.2.19)는 단백질의 lysine 잔기에 ubiquitin 분자를 붙여준다. H2A 히스톤의 ubiquitination은 유전자 침묵과 관련이 있다.

	Cat. No.	Product	Activity
Ubiquitin E3 Ligase Inhibitors	5397	A01	High affinity Smurf1 inhibitor; enhances BMP signaling
	5747	Apcin	Cdc20 inhibitor; inhibits Cdc20-substrate interaction
	5636	GS 143	β-TrCP1 ligase inhibitor
	5433	Heclin	HECT E3 ubiquitin ligase inhibitor
	3503	HLI 373	Hdm2 inhibitor; activates p53-dependent transcription
	6904	Idasanutlin	Potent MDM2 inhibitor; inhibits MDM2-p53 interaction
	7289	Nimbolide	RNF114 inhibitor
	3984	Nutlin-3	MDM2 antagonist; inhibits MDM2-p53 interaction
	6075	Nutlin 3a	MDM2 antagonist; active enantiomer of Nutlin-3 (Cat. No. 3984)
	5047	PRT 4165	Inhibitor of Bmi1/Ring1A; blocks histone H2A ubiquitination
	5191	PTC 209	Bmi-1 inhibitor; antitumor
	2443	RITA	MDM2-p53 interaction inhibitor
	4817	SKPin C1	Inhibits Skp2-mediated p27 degradation; induces cell cycle arrest
	4375	SMER 3	Selective inhibitor of E3 ubiquitin ligase
	7192	SMIP 004	SKP2 (S-phase kinase-associated protein 2) inhibitor; upregulates p27 and arrests cell cycle in G1 phase
	5332	SP 141	High affinity MDM2 inhibitor
	5076	SZL P1-41	Selective Skp2 inhibitor; suppresses E3 ligase activity
	652	Thalidomide	Binds cereblon; also TNF-α synthesis inhibitor
	6156	VH 298	High-affinity inhibitor of VHL
	7055	WS 383	Potent, selective and reversible DCN1-UBC12 interaction inhibitor
	6719	YH 239-EE	MDM2 inhibitor; disrupts MDM2-p53 interaction
Degraders	6416	CM 11	Homo-PROTAC® for self-degradation of pVHL30
	7219	CRBN PROTAC® 14a	Cereblon Degrader (PROTAC®)
	6948	CRBN-6-5-5-VHL	Potent and selective cereblon Degrader; cell-permeable
Controls	6157	cis VH 298	Negative control for VH 298
Others	7287	FAM-DEALA-Hyp-YIPD	Fluorescent HIF-1α peptide; can be used to evaluate the effect of VHL binding on degradation activity
	7452	FAM-DEALAHypYIPMDDDFQLRSF	Fluorescent HIF-1α peptide; can be used to evaluate the effect of VHL binding on degradation activity
	6782	Indisulam	Molecular glue; pre-mRNA splicing modulator
	6305	Lenalidomide	Cereblon binder; induces ubiquitination and degradation of CK1α by E3 ubiquitin ligase
	5131	NAB 2	Protects against α-synuclein toxicity; promotes Rsp5/Nedd4-dependent endosomal transport
	6302	Pomalidomide	Cereblon binder; also TNF-α inhibitor and antiangiogenic
	3365	Tenovin-1	Protects against MDM2-mediated p53 degradation
	7288	Thalidomide-Cyanine 5	High affinity cereblon fluorescent probe

DNA methylation

DNA methyltransferase(DNMTs)는 이중나선의 major groove에 있는 뉴클레오티드에 메틸기를 추가해서 전사인자와 중합효소가 결합하는 것을 막아 전사를 억제한다.

	Cat. No.	Product	Activity
DNA Methyltransferase Inhibitors	3842	5-Azacytidine	DNA methyltransferase inhibitor
	2624	Decitabine	DNA methyltransferase inhibitor
	4524	EGCG	DNMT1 inhibitor
	5016	Fisetin	DNMT1 inhibitor
	4359	Lomeguatrib	MGMT inhibitor
	3295	RG 108	Non-nucleoside DNA methyltransferase inhibitor
	5155	SGI 1027	DNA methyltransferase inhibitor
	2293	Zebularine	DNA methyltransferase and cytidine deaminase inhibitor
Others	1745	5-Iodotubercidin	Potent adenosine kinase inhibitor; decreases DNA methylation
	6615	KCC 07	MBD2 (Methyl-CpG-binding domain protein 2) inhibitor
	4061	6-Thioguanine	Anticancer and immunosuppressive agent; disrupts cytosine methylation

주문정보

주문정보 - Cat No, PRODUCT, SIZE, 수량 등 항목으로 구성되어있습니다.
	Product	Cat.No.	Size	Maker	Qty	Data Sheet	MSDS

전체보기

1
Maker
Cat.No.
Product
Size
Qty
Data Sheet
MSDS

Epigenetic Writers Inhibitor & Activator | 고마바이오텍

Antibody

주문정보

추천제품

관련제품

자료

웨비나/Video

제품 문의

로그인