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Immune Checkpoint Inhibitors | Cytokine Inhibitor 이미지

Immune Checkpoint Inhibitors | Cytokine Inhibitor

Immune Checkpoints, mTOR, Cytokines, Checkpoint Control Kinases에 대한 small molecule을 소개합니다.

Immune Checkpoints 

 

  • Immune checkpoint molecule은 면역억제 신호경로에 관여하여 면역세포의 활성을 유도합니다.
  • indoleamine 2,3-dioxygenase (IDO), tryptophan 2,3 dioxygenase (TDO), arginase 와 같은 특정 대사 효소도 면역세포 기능에 필수적인 아미노산을 국소적으로 고갈시키는 역할을 하므로 Immune checkpoint molecule로 간주됩니다. 

 

Cat. No. Product Name Activity
6515 (D)-PPA 1 PD-1/PD-L1 interaction inhibitor
1545 (R)-(+)-Bay K 8644 TMEM176B inhibitor; activates inflammasomes; also CaV1.x blocker
5698 1-Methyl-D-tryptophan Indoleamine 2,3-dioxygenase (IDO) inhibitor
4392 680C91 Potent and selective tryptophan 2,3-dioxygenase (TDO) inhibitor
7831 AUNP 12 Peptide inhibitor of the PD-1 signaling pathway
6007 INCB 024360-analog Potent indoleamine 2,3-dioxygenase (IDO) inhibitor
6068 Lin28 1632 Lin28 inhibitor; suppresses PD-L1 expression and enhances T cell-mediated antitumor immunity; also bromodomain inhibitor
8119 ML T7 Inhibitor of phosphatidylserine/CEACAM1 binding to Tim-3
6370 Nor NOHA monoacetate Arginase inhibitor
8050 SA-15-P Dual inhibitor of LAG3 interaction with both MHCII and FGL1
6979 SEN 177 Disrupts binding of SIRP-α to CD47; potent glutaminyl cyclase inhibitor.
7533 ZE 132 Potent and selective PD-1/PD-L1 interaction inhibitor

 

 

Checkpoint Control Kinases

 

  • Checkpoint control kinase는 세포 주기를 통해 세포의 진행을 조절하는 효소 그룹을 말합니다. 이전 단계가 완료되기 전에 세포주기의 다음 단계로 진행되면 치명적인 유전적 손상이 발생할 수 있습니다.

Cat. No.Product Activity
5198AZ 20Potent and selective ATR kinase inhibitor; antitumor
3994AZ 3146Potent and selective Mps1 inhibitor
6330AZ 5704Potent and selective ATM kinase inhibitor; orally bioavailable.
5199AZD 7762 hydrochloridePotent and selective ATP-competitive inhibitor of Chk1 and Chk2
4968CCT 241533 dihydrochloridePotent Chk2 inhibitor
4840KU 0060648Dual DNA-PK and PI 3-K inhibitor
3544KU 55933Potent and selective ATM kinase inhibitor
6454LY 2603618Potent and selective Chk1 inhibitor
3190MirinMRN-ATM pathway inhibitor
5142Mps1-IN-1 dihydrochlorideSelective Mps1 kinase inhibitor
3034NSC 109555 ditosylateSelective Chk2 inhibitor
2828NU 7026Selective DNA-PK inhibitor
3712NU 7441Potent and selective DNA-PK inhibitor
3785PD 166285 dihydrochlorideWee1 inhibitor; also inhibits Src, FGFR and PDGFRβ
2694PD 407824Potent and selective inhibitor of Chk1 and Wee1
4277PF 477736Selective Chk1 inhibitor
2930PI 103 hydrochlorideInhibitor of DNA-PK, mTOR and PI 3-kinase
2560SB 218078Chk1 inhibitor
4750TC Mps1 12Potent and selective Mps1 kinase inhibitor; orally active
3038TCS 2312Potent Chk1 inhibitor

 

  

mTOR


  • mTOR는 세포 신호 전달 경로를 조정하는데 중요한 역할을 합니다.
  • mTOR는 분자량 280kD이상의 large multidomain protein으로 kinase domain과 FKBP12 binding domain을 갖고 있습니다.

Cat. No.Product NameActivity
5615AZD 3147Potent and selective dual mTORC1 and 2 inhibitor; orally bioavailable
6791BC-LI-0186Inhibits mTORC1 activity; TRS/Ras-related GTP-binding protein D (RagD) interaction inhibitor
5955eCF 309Potent mTOR inhibitor
4702ETP 45658mTOR inhibitor; also inhibits PI 3-K and DNA-PK
6188EverolimusmTOR inhibitor; Immunosuppressant
3725KU 0063794Selective mTOR inhibitor
4079NiclosamideSTAT3 inhibitor; also inhibits mTORC1 signaling
6792OmipalisibHigh affinity mTOR inhibitor; also highly potent PI 3-kinase and potent DNA-PK inhibitor
4820PF 04691502Dual PI 3-K/mTOR inhibitor
4823PF 05212384Potent and selective dual PI 3-kinase/mTOR inhibitor
2930PI 103 hydrochlorideInhibitor of mTOR, PI 3-kinase and DNA-PK
3894PP 121Dual kinase inhibitor; inhibits PI 3K family kinases
4257PP 242Dual mTORC1/mTORC2 inhibitor
1292RapamycinmTOR inhibitor; immunosuppressant
6036STK16-IN-1mTOR kinase inhibitor; also inhibits PI 3Kδ, PI 3Kγ and STK16 kinases
5264TemsirolimusmTOR inhibitor; antitumor
4247Torin 1Potent and selective mTOR inhibitor
4248Torin 2Potent and selective mTOR inhibitor
4282WYE 687 dihydrochloridePotent and selective mTOR inhibitor
4893XL 388Potent and selective mTOR inhibitor; antitumor
 

 

Akt(Protein Kinase B)

 

  • Akt (Protein kinase B, PKB)는 세포의 생존, 혈관 신생, 종양 형성을 조절하는데 중요한 역할을 하는 serine/threonine kinase 입니다.

Cat. No.Product NameActivity
255810-DEBC hydrochlorideSelective Akt/PKB inhibitor
5985AKT Inhibitor IV Promotes Akt hyperphosphorylation; decreases phosphorylation of Akt substrates
1353Akt/SKG Substrate PeptideAkt/PKB substrate (synthetic)
5773Akti-1/2Potent and selective dual Akt1 and 2 inhibitor
3897API-1Selective Akt/PKB inhibitor. Antitumor
2151API-2Selective inhibitor of Akt/PKB signaling. Antitumor and antiviral
7001AT 7867Potent pan-Akt and PKA inhibitor
6978AZD 5363Potent pan-AKT inhibitor
2926FPA 124Akt/PKB inhibitor
4144GSK 690693Akt kinase inhibitor. Antitumor
5682OSU 03012Akt signaling inhibitor; inhibits PDPK1 (PDK1)
6087PerifosinePKB/Akt inhibitor; also modulates Kv2.1 current
4598PHT 427Dual Akt and PDK1 inhibitor; antitumor
4398SC 66Allosteric Akt inhibitor
4635SC 79Akt activator
6762Urolithin API 3-K/Akt/mTOR signaling inhibitor; blocks phosphorylation of Akt and p70S6K in vitro

  

 

Cytokines

 

  • Cytokine은 면역반응의 주요 매개체인 단백질성 신호 화합물 입니다.
  • 증식, 분화, 세포생존 및 apoptosis를 포함하여 다양한 세포 기능을 제어하며, 여러 병리생리학적 과정에도 관여합니다.

Cat. No.Product NameActivity
4400(±)-CPSI 1306Reported macrophage migration inhibitory factor (MIF) inhibitor
4656(D)-(+)-NeopterinStimulated by IFN-γ; marker of immune activation
6829(R)-ShikoninBlocks TNF-α and NF-κB signaling; induces necroptosis; anti-inflammatory
34294-IPPInhibitor of macrophage migration inhibitory factor (MIF); suicide substrate
7283Apilimod dimesylateInhibits production of IL-12 and IL-23; potent and selective PIKfyve inhibitor
2446AS 101Immunomodulator; inhibits IL-10 synthesis and potentiates IL-1α, IL-2 and TNF-α release
5430AS 2444697Potent and selective IRAK4 inhibitor
6438BRD 6989IL-10 production enhancer; Cdk8 inhibitor
4316BropirimineImmunomodulatory and antitumor compound
4204BTZO 1MIF binder
5484C 87TNF-α inhibitor
0846Chicago Sky Blue 6BMIF inhibitor; also inhibits L-glutamate uptake into synaptic vesicles
6107CP 424174Inhibitor of IL-1β post-translational processing; indirectly inhibits NLRP3
5479CRID3 sodium saltPotent NLRP3 inflammasome inhibitor; inhibits IL-1β production
2471ER 27319 maleateInhibits TNF-α production
1798Gabexate mesylateInhibits TNF-α production. Also antithrombotic agent
3270GIT 27Immunomodulator; reduces production of pro-inflammatory cytokines
5126iMDKSuppressor of MDK expression; inhibits PI 3-K signaling
4288ISO 1Macrophage migration inhibitory factor (MIF) inhibitor
5185JTE 607 dihydrochlorideCytokine release inhibitor; anti-inflammatory
6305LenalidomideTNF-α inhibitor; inhibits angiogenesis; also cereblon binder
6373PF 06650833Potent and selective IRAK4 inhibitor
1093PirfenidoneAntifibrotic agent; regulates cytokine levels in vivo
6302PomalidomideTNF-α inhibitor; also cereblon ubiquitination inhibitor and antiangiogenic
7066RCGD 423gp130 modulator; activates JAK/STAT signaling
4963SC 144 hydrochloridegp130 inhibitor; blocks cytokine-triggered gp130 signaling
0652ThalidomideTNF-α synthesis inhibitor; also binds cereblon
6583UCLA GP130 2gp130 agonist; brain penetrant and neuroprotectant
 

 

주문정보

주문정보 - Cat No, PRODUCT, SIZE, 수량 등 항목으로 구성되어있습니다.
  Product Cat.No. Size Maker Qty Data Sheet MSDS
AUNP 12 7831 1 mg TOCRIS
BAY 1816032 7549 10 mg TOCRIS
(+/-)-CPSI 1306 (10 mg) 4400 10 mg TOCRIS
(D)-PPA 1 (1 MG) 6515 1 mg TOCRIS
(R)-(+)-Bay K 8644 (10 mg) 1545 10 mg TOCRIS
(R)-(+)-Bay K 8644 (50 mg) 1545 50 mg TOCRIS
10-DEBC hydrochloride (10 mg) 2558 10 mg TOCRIS
10-DEBC hydrochloride (50 mg) 2558 50 mg TOCRIS
4-IPP (10 mg) 3429 10 mg TOCRIS
4-IPP (50 mg) 3429 50 mg TOCRIS
Adavosertib 7589 50 mg TOCRIS
Adavosertib 7589 10 mg TOCRIS
AKT Inhibitor IV 5985 5 mg TOCRIS
API-2 (10 mg) 2151 10 mg TOCRIS
AS 2444697 (10 mg) 5430 10 mg TOCRIS
AS 2444697 (50 mg) 5430 50 mg TOCRIS
AT 7867 (10 MG) 7001 10 mg TOCRIS
AT 7867 (50 MG) 7001 50 mg TOCRIS
AZ 20 (10 mg) 5198 10 mg TOCRIS
AZ 20 (50 mg) 5198 50 mg TOCRIS
AZ 3146 (10 mg) 3994 10 mg TOCRIS
AZ 3146 (50 mg) 3994 50 mg TOCRIS
AZ 5704 (25 MG) 6330 25 mg TOCRIS
AZ 5704 (5 MG) 6330 5 mg TOCRIS
AZD 5363 (25 MG) 6978 25 mg TOCRIS
AZD 5363 (5 MG) 6978 5 mg TOCRIS
BRD 6989 (10 MG) 6438 10 mg TOCRIS
BRD 6989 (50 MG) 6438 50 mg TOCRIS
Bropirimine (10 mg) 4316 10 mg TOCRIS
Bropirimine (50 mg) 4316 50 mg TOCRIS
BTZO 1 (10 mg) 4204 10 mg TOCRIS
BTZO 1 (50 mg) 4204 50 mg TOCRIS
CCT 241533 dihydrochloride (10 mg) 4968 10 mg TOCRIS
Compound 401 (10 mg) 3271 10 mg TOCRIS
CRID3 sodium salt (10 mg) 5479 10 mg TOCRIS
CRID3 sodium salt (50 mg) 5479 50 mg TOCRIS
Dexamethasone 11-082 5 g PROSCI
ER 27319 maleate (10 mg) 2471 10 mg TOCRIS
ER 27319 maleate (50 mg) 2471 50 mg TOCRIS
Everolimus (10 MG) 6188 10 mg TOCRIS
FPA 124 (10 mg) 2926 10 mg TOCRIS
FPA 124 (50 mg) 2926 50 mg TOCRIS
Gabexate mesylate (10 mg) 1798 10 mg TOCRIS
Gabexate mesylate (50 mg) 1798 50 mg TOCRIS
GSK 690693 (10 mg) 4144 10 mg TOCRIS
iMDK (10 mg) 5126 10 mg TOCRIS
iMDK (50 mg) 5126 50 mg TOCRIS
ISO 1 (10 mg) 4288 10 mg TOCRIS
ISO 1 (50 mg) 4288 50 mg TOCRIS
JTE 607 dihydrochloride (10 mg) 5185 10 mg TOCRIS
전체보기
Maker
TOCRIS
Cat.No.
7831
Product
AUNP 12
Size
1 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
7549
Product
BAY 1816032
Size
10 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
4400
Product
(+/-)-CPSI 1306 (10 mg)
Size
10 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
6515
Product
(D)-PPA 1 (1 MG)
Size
1 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
1545
Product
(R)-(+)-Bay K 8644 (10 mg)
Size
10 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
1545
Product
(R)-(+)-Bay K 8644 (50 mg)
Size
50 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
2558
Product
10-DEBC hydrochloride (10 mg)
Size
10 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
2558
Product
10-DEBC hydrochloride (50 mg)
Size
50 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
3429
Product
4-IPP (10 mg)
Size
10 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
3429
Product
4-IPP (50 mg)
Size
50 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
7589
Product
Adavosertib
Size
50 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
7589
Product
Adavosertib
Size
10 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
5985
Product
AKT Inhibitor IV
Size
5 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
2151
Product
API-2 (10 mg)
Size
10 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
5430
Product
AS 2444697 (10 mg)
Size
10 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
5430
Product
AS 2444697 (50 mg)
Size
50 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
7001
Product
AT 7867 (10 MG)
Size
10 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
7001
Product
AT 7867 (50 MG)
Size
50 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
5198
Product
AZ 20 (10 mg)
Size
10 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
5198
Product
AZ 20 (50 mg)
Size
50 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
3994
Product
AZ 3146 (10 mg)
Size
10 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
3994
Product
AZ 3146 (50 mg)
Size
50 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
6330
Product
AZ 5704 (25 MG)
Size
25 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
6330
Product
AZ 5704 (5 MG)
Size
5 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
6978
Product
AZD 5363 (25 MG)
Size
25 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
6978
Product
AZD 5363 (5 MG)
Size
5 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
6438
Product
BRD 6989 (10 MG)
Size
10 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
6438
Product
BRD 6989 (50 MG)
Size
50 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
4316
Product
Bropirimine (10 mg)
Size
10 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
4316
Product
Bropirimine (50 mg)
Size
50 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
4204
Product
BTZO 1 (10 mg)
Size
10 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
4204
Product
BTZO 1 (50 mg)
Size
50 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
4968
Product
CCT 241533 dihydrochloride (10 mg)
Size
10 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
3271
Product
Compound 401 (10 mg)
Size
10 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
5479
Product
CRID3 sodium salt (10 mg)
Size
10 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
5479
Product
CRID3 sodium salt (50 mg)
Size
50 mg
Qty
Data Sheet
MSDS
Maker
PROSCI
Cat.No.
11-082
Product
Dexamethasone
Size
5 g
Qty
Data Sheet
Maker
TOCRIS
Cat.No.
2471
Product
ER 27319 maleate (10 mg)
Size
10 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
2471
Product
ER 27319 maleate (50 mg)
Size
50 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
6188
Product
Everolimus (10 MG)
Size
10 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
2926
Product
FPA 124 (10 mg)
Size
10 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
2926
Product
FPA 124 (50 mg)
Size
50 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
1798
Product
Gabexate mesylate (10 mg)
Size
10 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
1798
Product
Gabexate mesylate (50 mg)
Size
50 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
4144
Product
GSK 690693 (10 mg)
Size
10 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
5126
Product
iMDK (10 mg)
Size
10 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
5126
Product
iMDK (50 mg)
Size
50 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
4288
Product
ISO 1 (10 mg)
Size
10 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
4288
Product
ISO 1 (50 mg)
Size
50 mg
Qty
Data Sheet
MSDS
Maker
TOCRIS
Cat.No.
5185
Product
JTE 607 dihydrochloride (10 mg)
Size
10 mg
Qty
Data Sheet
MSDS
전체보기

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0.5 ml Elite Pre-stained Protein Ladder (2 x 0.25 ml) PAL-EPL-500 0.5ml 500
Maker
Cat.No.
Product
Size
Qty
Data Sheet
MSDS

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