| 14.3.3 Proteins Inhibitors |
|
| 14.3.3 단백질은 대사, 단백질 trafficking, 신호 전달, 세포 사멸 및 세포 주기 조절과 같은 많은
중요한 세포 과정에 관여하는 고도로 보존된 단백질 그룹입니다. 14.3.3 단백질은 phospho-serine/-threonine
binding protein 입니다. |
| Cat. No. |
Product Name |
Activity |
| 2144 |
R18 |
Inhibitor of 14.3.3 proteins |
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| Apoptosis Inducers |
|
| 아폽토시스를 유도하는 inducer는 DNA cross-linking, anti-apoptosis 단백질 억제 및
caspase의 활성화를 포함한 다양한 메커니즘을 통해 pro-apoptosis 효과를 나타냅니다. 이러한 유도제는 antitumor 또는
antineoplastic effect를 유도하기 위해 특정 세포 과정을 표적으로 할 수 있습니다. |
| Cat. No. |
Product Name |
Activity |
| 0789 |
(±)-Anatoxin A fumarate |
nAChR agonist; apoptosis inducer |
| 2137 |
2,3-DCPE hydrochloride |
Selectively induces cancer cell apoptosis |
| 1229 |
Actinomycin D |
Antineoplastic antibiotic |
| 2098 |
Apoptosis Activator 2 |
Selectively induces tumor cell apoptosis |
| 3367 |
AT 101 |
Downregulates Bcl-2 and Mcl-1; pro-apoptotic |
| 3681 |
Bendamustine hydrochloride |
Cytostatic agent; exhibits DNA alkylating and purine analog
properties |
| 3906 |
Betulinic acid |
Antitumor and anti-HIV agent; activates NF-κB. Also TGR5 agonist |
| 5791 |
Bz 423 |
ATP synthase inhibitor; proapoptotic |
| 2489 |
C 75 |
Induces apoptosis and exhibits anti-tumor activity |
| 2626 |
Carboplatin |
DNA cross-linking antitumor agent |
| 5804 |
Chaetoglobosin A |
Selectively induces apoptosis of CLL cells; antibiotic |
| 2251 |
Cisplatin |
DNA-alkylating antitumor agent |
| 5292 |
Cladribine |
Deoxyadenosine analog; pro-apoptotic |
| 4091 |
Cyclophosphamide |
Alkylating agent; chemotherapeutic |
| 2252 |
Doxorubicin hydrochloride |
Antitumor antibiotic agent; induces apoptosis |
| 7507 |
Evofosfamide |
Hypoxia-activated DNA alkylating agent prodrug |
| 4808 |
FK 866 hydrochloride |
Potent and non-competitive NAMPT inhibitor; induces apoptosis
and autophagy |
| 3495 |
Fludarabine |
Proapoptotic; increases Bax and decreases Bid, XIAP and survivin
expression |
| 6776 |
G5 |
Activates apoptosis in an apoptosome-independent pathway;
ubiquitin isopeptidase inhibitor |
| 3603 |
Kaempferol |
Proapoptotic; downregulates PLK1 expression and activates
mitochondrial Ca2+ uniporter |
| 6617 |
LYN 1604 dihydrochloride |
Induces apoptosis; ULK1 agonist |
| 3258 |
Mitomycin C |
DNA cross-linking antitumor agent |
| 5231 |
MPC 6827 hydrochloride |
Inhibitor of microtubule polymerization; antimitotic and
antitumor |
| 3715 |
Narciclasine |
Antiproliferative agent; exhibits pro-apoptotic effects |
| 3427 |
Oncrasin 1 |
Proapoptotic; induces abnormal nuclear accumulation of PKCι |
| 2623 |
Oxaliplatin |
DNA cross-linking antitumor agent |
| 4643 |
PCI 34051 |
Potent and selective histone deacetylase 8 inhibitor; induces
apoptosis in T cell-derived cell lines |
| 5359 |
Rifaximin |
Apoptosis inducer; pregnane X receptor agonist and antibiotic |
| 5314 |
SMBA 1 |
High affinity and selective activator of Bax |
| 1621 |
Streptozocin |
DNA alkylator; antitumor and induces diabetes |
| 2706 |
Temozolomide |
DNA-methylating antitumor agent |
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|
| ASK1 Inhibitors |
|
| Apoptosis signal-regulated kinase 1 (ASK1)은 serine/threonine
kinase, MAP3K family member로 JNK와 p38의 활성을 통해 apoptosis를 유도합니다. ASK1은 신경퇴행성
질환과 산화스트레스 관련 질병의 병리학적인 부분에 관여합니다. |
| Cat. No. |
Product Name |
Activity |
| 5641 |
MSC 2032964A |
Potent and selective ASK1 inhibitor; orally bioavailable |
| 4825 |
TC ASK 10 |
Potent and selective ASK1 inhibitor; orally bioavailable |
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| Bcl-2 Family
Inhibitors & Activators |
|
| Bcl-2 Family는 apoptosis의 programmed cell death에 관여하며 모든 구성요소들은
4개의 Bcl-2 homology domain 중 적어도 하나를 갖고 있습니다. Bcl-2, Bcl-XL, Mcl-1과 같은 요소들은
anti-apoptotic 역할을, Bax, Bak, Bok등은 proapoptotic 역할을 합니다. |
| Cat. No. |
Product Name |
Activity |
| 6409 |
A 1210477 |
Selective, high affinity Mcl-1 inhibitor; proapoptotic |
| 7661 |
A 1331852 |
Potent and selective Bcl-xL inhibitor; antitumor and inducer of
apoptosis |
| 6960 |
ABT 199 |
Selective, high affinity Bcl-2 inhibitor; orally bioavailable |
| 7680 |
ABT 263 |
High affinity Bcl-2 family inhibitor; proapoptotic, senolytic
and antitumor |
| 6835 |
ABT 737 |
Bcl-2 family inhibitor; mimics BH3 and induces apoptosis in
cancer cell lines |
| 4676 |
ARRY 520 trifluoroacetate |
Potent and selective kinesin spindle protein (KSP) inhibitor;
induces Mcl-1 degradation |
| 2160 |
Bax channel blocker |
Allosteric inhibitor of Bax channel activation |
| 6323 |
FX 1 |
Bcl-6 inhibitor; 10-fold more potent than endogenous Bcl-6
corepressors |
| 3794 |
iMAC2 |
Inhibitor of Bid-induced Bax cytochrome c release |
| 4819 |
Methylprednisolone |
Anti-apoptotic; upregulates expression of Bcl-xL after injury |
| 5733 |
ML 311 |
Inhibits Mcl-1-BIM interaction |
| 6539 |
Obatoclax mesylate |
Inhibitor of Bcl-2 family members; antiapoptotic |
| 5314 |
SMBA 1 |
High affinity and selective activator of Bax |
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| Calpain Inhibitors |
|
| Calpain은 calcium-sensitive cysteine proteases 그룹에 속하며 포유류에서
어느곳에서나 발현합니다. 구조적으로 80kDa catalytic subunit와 28kDa regulatory subunit를
가집니다. |
| Cat. No. |
Product Name |
Activity |
| 2950 |
Acetyl-Calpastatin (184-210) (human) |
Selective calpain inhibitor |
| 0448 |
Calpeptin |
Calpain and cathepsin L inhibitor |
| 5208 |
E 64 |
Potent and irreversible cysteine protease inhibitor |
| 1748 |
MG 132 |
Proteasome and calpain inhibitor. Inhibits NF-κB activation |
| 1269 |
PD 150606 |
Cell permeable calpain inhibitor |
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| Caspase Inhibitors
& Activators |
|
| Caspases (cysteinyl aspartate proteases)는 apoptosis, necrosis,
inflammation의 시그널링에 관여하는 효소로 initiator와 effector로 구분됩니다. Initiator isoform은
upstream adaptor molecule에 의해 활성화되고 반응합니다. |
| Cat. No. |
Product Name |
Activity |
| 7242 |
Ac-FLTD-CMK |
Potent and selective inhibitor of caspases 1, 5 and 4 |
| 2251 |
Cisplatin |
Potent pro-apoptotic anticancer agent; activates caspase-3 |
| 7310 |
Emricasan |
Potent pan-caspase inhibitor |
| 6172 |
INF 4E |
Caspase-1 and NLRP3 inflammasome inhibitor |
| 2581 |
PAC 1 |
Activator of procaspase-3; pro-apoptotic |
| 7143 |
VX 765 |
High affinity and selective caspase-4 and caspase 1/ICE
inhibitor; orally bioavailable |
| 2166 |
Z-DEVD-FMK |
Cell-permeable, irreversible caspase-3 inhibitor |
| 2163 |
Z-VAD-FMK |
Cell-permeable, irreversible caspase inhibitor |
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|
| Inhibitor of
Apoptosis Inhibitors |
|
| The inhibitor of apoptosis (IAP) family는 apoptosis caspase를 유도하는
인자들과 함께 apoptosis의 대표 regulator 입니다. |
| Cat. No. |
Product Name |
Activity |
| 6470 |
A 410099.1 |
High affinity XIAP antagonist; active in
vivo |
| 5141 |
AZD 5582 dihydrochloride |
Dimeric Smac mimetic; potent IAP inhibitor |
| 5251 |
UC 112 |
IAP and XIAP inhibitor; antitumor |
| 6491 |
YM 155 |
Survivin suppressor |
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| p53 Inhibitors |
|
| p53은 단백질 레벨과 post-translational modification state가 세포스트레스 (예,
저산소증, DNA 및 spindle 손상 등..)에 반응하여 변경되는 전사인자 입니다. p53의 활성화는 ATM, ATR, Chk1,
MAPK에 의한 인산화를 포함한 여러 메커니즘에 의해 발생합니다. |
| Cat. No. |
Product Name |
Activity |
| 3843 |
Cyclic Pifithrin-α hydrobromide |
p53 inhibitor |
| 3503 |
HLI 373 |
Hdm2 inhibitor; activates p53-dependent transcription |
| 6904 |
Idasanutlin |
Potent MDM2 inhibitor; inhibits MDM2-p53 interaction |
| 6615 |
KCC 07 |
BAI1/p53 signaling activator; inhibits MBD2 (Methyl-CpG-binding
domain protein 2) |
| 2185 |
NSC 146109 hydrochloride |
Cell-permeable, genotype-selective antitumor agent; activates
p53-dependent transcription |
| 5065 |
NSC 319726 |
Reactivator of mutant p53 |
| 6075 |
Nutlin 3a |
MDM2 antagonist; active enantiomer of Nutlin-3 (Cat.
No. 3984) |
| 3984 |
Nutlin-3 |
MDM2 antagonist; inhibits MDM2-p53 interaction |
| 1267 |
Pifithrin-α hydrobromide |
p53 inhibitor. Also aryl hydrocarbon receptor agonist |
| 2653 |
Pifithrin-μ |
Inhibitor of p53-mitochondrial binding |
| 2443 |
RITA |
p53-MDM2 interaction inhibitor; antitumor |
| 5332 |
SP 141 |
High affinity MDM2 inhibitor |
| 3356 |
WR 1065 dihydrochloride |
p53 activator. Also ROS scavenger |