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MedKoo Cat#: 585025 | Name: SKLB-23bb
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

SKLB-23bb, also known as HDAC6-IN-1, is an orally bioavailable HDAC6-selective inhibitor and also has microtubule-disrupting ability.

Chemical Structure

SKLB-23bb
SKLB-23bb
CAS#1815580-06-3

Theoretical Analysis

MedKoo Cat#: 585025

Name: SKLB-23bb

CAS#: 1815580-06-3

Chemical Formula: C21H24N4O4

Exact Mass: 396.1798

Molecular Weight: 396.45

Elemental Analysis: C, 63.62; H, 6.10; N, 14.13; O, 16.14

Price and Availability

Size Price Availability Quantity
1mg USD 450.00 2 Weeks
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Related CAS #
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Synonym
SKLB-23bb; SKLB 23bb; SKLB23bb; HDAC6-IN-1;
IUPAC/Chemical Name
Butanamide, N-hydroxy-4-[2-methoxy-5-[methyl(2-methyl-4-quinazolinyl)amino]phenoxy]-
InChi Key
FWXZZFONXWYSEF-UHFFFAOYSA-N
InChi Code
InChI=1S/C21H24N4O4/c1-14-22-17-8-5-4-7-16(17)21(23-14)25(2)15-10-11-18(28-3)19(13-15)29-12-6-9-20(26)24-27/h4-5,7-8,10-11,13,27H,6,9,12H2,1-3H3,(H,24,26)
SMILES Code
O=C(NO)CCCOC1=CC(N(C)C2=C3C=CC=CC3=NC(C)=N2)=CC=C1OC
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
SKLB-23bb is an inhibitor of histone deacetylase 6 (HDAC6; IC50 = 17 nM). It is selective for HDAC6 over HDAC1-5 and HDAC7-11 (IC50s = 386->10,000 nM). SKLB-23bb inhibits tubulin acetylation in HeLa cervical cancer cells (EC50 = 58.9 nM) and the proliferation of A375 melanoma and HeLa cells (IC50s = 45 and 49 nM, respectively). It also binds to the colchicine site in β-tubulin and inhibits microtubule formation in MDA-MB-231 cells.
In vitro activity:
SKLB-23bb is a potent oral anticancer candidate for selective HDAC6 inhibitor. In vitro, SKLB-23bb presented low nanomolar antiproliferative effects against a panel of cancer cell lines. Western blot analysis confirmed that SKLB-23bb increased acetylation level of α-tubulin. Reference: J Med Chem. 2016 Feb 25;59(4):1455-70. https://pubmed.ncbi.nlm.nih.gov/26443078/
In vivo activity:
In solid tumor xenografts, oral administration of SKLB-23bb efficiently inhibited tumor growth, suggesting that SKLB-23bb was an orally bioavailable HDAC6 and microtubule dual targeting agent. Reference: Mol Cancer Ther. 2018 Apr;17(4):763-775. https://pubmed.ncbi.nlm.nih.gov/29610282/
Solvent mg/mL mM comments
Solubility
DMSO 79.0 199.27
Water 79.0 199.27
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 396.45 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Yang Z, Wang T, Wang F, Niu T, Liu Z, Chen X, Long C, Tang M, Cao D, Wang X, Xiang W, Yi Y, Ma L, You J, Chen L. Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. J Med Chem. 2016 Feb 25;59(4):1455-70. doi: 10.1021/acs.jmedchem.5b01342. Epub 2015 Oct 13. PMID: 26443078. 2. Wang F, Zheng L, Yi Y, Yang Z, Qiu Q, Wang X, Yan W, Bai P, Yang J, Li D, Pei H, Niu T, Ye H, Nie C, Hu Y, Yang S, Wei Y, Chen L. SKLB-23bb, A HDAC6-Selective Inhibitor, Exhibits Superior and Broad-Spectrum Antitumor Activity via Additionally Targeting Microtubules. Mol Cancer Ther. 2018 Apr;17(4):763-775. doi: 10.1158/1535-7163.MCT-17-0332. PMID: 29610282.
In vitro protocol:
1. Yang Z, Wang T, Wang F, Niu T, Liu Z, Chen X, Long C, Tang M, Cao D, Wang X, Xiang W, Yi Y, Ma L, You J, Chen L. Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. J Med Chem. 2016 Feb 25;59(4):1455-70. doi: 10.1021/acs.jmedchem.5b01342. Epub 2015 Oct 13. PMID: 26443078.
In vivo protocol:
1. Wang F, Zheng L, Yi Y, Yang Z, Qiu Q, Wang X, Yan W, Bai P, Yang J, Li D, Pei H, Niu T, Ye H, Nie C, Hu Y, Yang S, Wei Y, Chen L. SKLB-23bb, A HDAC6-Selective Inhibitor, Exhibits Superior and Broad-Spectrum Antitumor Activity via Additionally Targeting Microtubules. Mol Cancer Ther. 2018 Apr;17(4):763-775. doi: 10.1158/1535-7163.MCT-17-0332. PMID: 29610282.
[1] Wang F, et al. Mol Cancer Ther. 2018, 17(4):763-775.